Biased Signaling Atlas

Ligand source activities (1 row/activity)

Potency
Affinity

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	AssayType	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	1324	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	16154396	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	16197727	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	44285019	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	57514683	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	91898441	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	CHEMBL441738	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	DB04931	302	25	None	-14	9	Human	10.8	pEC50	=	10.8	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
	CHEMBL413212	213055	0	None	3	4	Human	10.7	pEC50	=	10.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	CHEMBL428615	213460	0	None	1	5	Human	10.7	pEC50	=	10.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	1324	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	16154396	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	16197727	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	44285019	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	57514683	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	91898441	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	CHEMBL441738	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	DB04931	302	25	None	-14	9	Human	10.7	pEC50	=	10.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		None	10.1021/jm030111j
	155527254	171250	0	None	-	1	Human	10.5	pEC50	=	10.5	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4460053	171250	0	None	-	1	Human	10.5	pEC50	=	10.5	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
	57646411	76921	0	None	-	1	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070245	76921	0	None	-	1	Human	10.4	pEC50	=	10.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	1323	2688	55	None	-1	8	Mouse	10.4	pEC50	=	10.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	92432	2688	55	None	-1	8	Mouse	10.4	pEC50	=	10.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	CHEMBL430239	2688	55	None	-1	8	Mouse	10.4	pEC50	=	10.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	1323	2688	55	None	-36	8	Human	10.4	pEC50	=	10.4	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	92432	2688	55	None	-36	8	Human	10.4	pEC50	=	10.4	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	CHEMBL430239	2688	55	None	-36	8	Human	10.4	pEC50	=	10.4	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	118722941	116242	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358549	116242	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722937	116238	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358545	116238	0	None	-1	4	Mouse	10.3	pEC50	=	10.3	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722933	116235	0	None	-1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358541	116235	0	None	-1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	1323	2688	55	None	-1	8	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	92432	2688	55	None	-1	8	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	CHEMBL430239	2688	55	None	-1	8	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	155551846	175134	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
	CHEMBL4569789	175134	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
	CHEMBL415661	213198	0	None	-	1	Human	10.2	pEC50	=	10.2	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL2371851	210139	0	None	-1	4	Mouse	10.2	pEC50	=	10.2	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O	10.1021/jm0490843
	118722944	116245	0	None	1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358552	116245	0	None	1	4	Mouse	10.2	pEC50	=	10.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	1323	2688	55	None	-1	8	Mouse	10.1	pEC50	=	10.1	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	92432	2688	55	None	-1	8	Mouse	10.1	pEC50	=	10.1	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	CHEMBL430239	2688	55	None	-1	8	Mouse	10.1	pEC50	=	10.1	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	44310104	81588	0	None	-4	4	Mouse	10.1	pEC50	=	10.1	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1040	16	13	13	-1.5	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303608
	CHEMBL216295	81588	0	None	-4	4	Mouse	10.1	pEC50	=	10.1	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1040	16	13	13	-1.5	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CC(=O)ONCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303608
	1324	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	16154396	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	16197727	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	44285019	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	57514683	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	91898441	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	CHEMBL441738	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	DB04931	302	25	None	-9	9	Mouse	10.0	pEC50	=	10.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm701093y
	118722930	116233	0	None	-1	4	Mouse	10.0	pEC50	=	10.0	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358539	116233	0	None	-1	4	Mouse	10.0	pEC50	=	10.0	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL412495	212998	0	None	-	1	Human	10.0	pEC50	=	10	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	16746823	18157	0	None	-	1	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269576	18157	0	None	-	1	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL2372570	210271	0	None	-1	4	Human	10.0	pEC50	=	10.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC2=NC=NC2)NC1=O	10.1021/jm9017866
	CHEMBL407809	212685	0	None	-	1	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	90643803	111743	0	None	-3	5	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	111743	0	None	-3	5	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	10408	720	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	5329	720	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	9941379	720	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	CHEMBL2070241	720	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	DB11653	720	28	None	-1	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	1323	2688	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	92432	2688	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	CHEMBL430239	2688	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	1323	2688	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	92432	2688	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	CHEMBL430239	2688	55	None	-36	8	Human	9.9	pEC50	=	9.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	118722926	116230	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3358535	116230	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	1324	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16154396	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16197727	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	44285019	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	57514683	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	91898441	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	CHEMBL441738	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	DB04931	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	1324	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	16154396	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	16197727	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	44285019	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	57514683	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	91898441	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	CHEMBL441738	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	DB04931	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		None	10.1021/jm0492756
	CHEMBL5090946	215285	0	None	-4	4	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	118722931	116234	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358540	116234	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	118722938	116239	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358546	116239	0	None	-1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCc2cn(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722942	116243	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358550	116243	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cn2cc(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	118722943	116244	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358551	116244	0	None	1	4	Mouse	9.9	pEC50	=	9.9	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1034	17	13	13	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	1324	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	16154396	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	16197727	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	44285019	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	57514683	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	91898441	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	CHEMBL441738	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	DB04931	302	25	None	-14	9	Human	9.9	pEC50	=	9.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		None	10.1021/jm201489a
	127036484	136445	0	None	-2	4	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735690	136445	0	None	-2	4	Mouse	9.9	pEC50	=	9.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	1324	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	16154396	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	16197727	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	44285019	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	57514683	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	91898441	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	CHEMBL441738	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	DB04931	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		None	10.1016/j.bmcl.2009.07.025
	1324	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	16154396	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	16197727	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	44285019	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	57514683	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	91898441	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	CHEMBL441738	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	DB04931	302	25	None	-9	9	Mouse	9.9	pEC50	=	9.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0490843
	57646437	76922	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684621	76922	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929804	76922	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070246	76922	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	127036484	136445	0	None	-2	4	Mouse	9.8	pEC50	=	9.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735690	136445	0	None	-2	4	Mouse	9.8	pEC50	=	9.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1024	17	14	11	-1.0	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL266879	210706	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0501432
	57646441	76920	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070243	76920	0	None	-	1	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL1688107	208834	0	None	1	4	Mouse	9.8	pEC50	=	9.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL5083551	214869	0	None	-10	4	Human	9.8	pEC50	=	9.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL2369484	209627	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL3646885	212023	0	None	74	2	Human	9.7	pEC50	=	9.7	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	118722927	116231	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3358536	116231	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCCCC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3287329	211311	0	None	1	5	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	16154396	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	16197727	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	44285019	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	57514683	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	91898441	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	CHEMBL441738	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	DB04931	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm501027w
	44415914	139270	0	None	5	3	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL379054	139270	0	None	5	3	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	10408	720	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	5329	720	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	9941379	720	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	CHEMBL2070241	720	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	DB11653	720	28	None	-1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
	1324	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	16154396	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	16197727	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	44285019	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	57514683	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	91898441	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	CHEMBL441738	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	DB04931	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm301253y
	1324	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	16154396	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	16197727	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	44285019	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	57514683	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	91898441	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	CHEMBL441738	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	DB04931	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/jm101425m
	1324	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16154396	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16197727	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	44285019	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	57514683	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	91898441	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL441738	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	DB04931	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL405087	212541	0	None	-1	5	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	1324	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	16154396	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	16197727	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	44285019	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	57514683	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	91898441	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	CHEMBL441738	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	DB04931	302	25	None	-14	9	Human	9.7	pEC50	=	9.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	CHEMBL2372859	210300	1	None	2	3	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O	10.1021/jm501027w
	90643808	111747	0	None	-14	5	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	1324	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	16154396	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	16197727	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	44285019	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	57514683	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	91898441	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	CHEMBL441738	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	DB04931	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		None	10.1021/jm010524p
	1324	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	16154396	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	16197727	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	44285019	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	57514683	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	91898441	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	CHEMBL441738	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	DB04931	302	25	None	-9	9	Mouse	9.7	pEC50	=	9.7	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303608
	16132144	209279	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	16133793	209279	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	44273719	209279	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	CHEMBL214332	209279	36	None	-12	8	Human	9.7	pEC50	=	9.7	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm00018a005
	CHEMBL5080489	214689	0	None	1	4	Human	9.7	pEC50	=	9.7	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	118722936	116237	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358544	116237	0	None	-1	4	Mouse	9.7	pEC50	=	9.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCc2cn(nn2)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	50899078	18154	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269573	18154	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL2373515	210379	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	90643802	111742	0	None	-14	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3646890	212028	0	None	72	2	Human	9.6	pEC50	=	9.6	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	10408	720	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	5329	720	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	9941379	720	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	CHEMBL2070241	720	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	DB11653	720	28	None	-1	4	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	56659456	63701	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801215	63701	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL408257	212704	0	None	2	2	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	90643804	111744	0	None	-8	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-8	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL264352	210617	0	None	-	1	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL1688107	208834	0	None	1	4	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL5087839	215120	0	None	2	3	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1324	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	16154396	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	16197727	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	44285019	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	57514683	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	91898441	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	CHEMBL441738	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	DB04931	302	25	None	-9	9	Mouse	9.6	pEC50	=	9.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00053
	CHEMBL267900	210737	0	None	5	2	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL491870	214077	0	None	-9	5	Human	9.6	pEC50	=	9.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	118722932	115518	0	None	-1	4	Mouse	9.5	pEC50	=	9.5	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3352878	115518	0	None	-1	4	Mouse	9.5	pEC50	=	9.5	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1038	33	13	11	1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	90643805	111745	0	None	1	5	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	111745	0	None	1	5	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	16154396	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	16197727	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	44285019	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	57514683	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	91898441	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	CHEMBL441738	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	DB04931	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030452x
	118735099	118799	0	None	4	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421676	118799	0	None	4	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	118735101	118801	0	None	9	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421678	118801	0	None	9	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	44415913	79951	0	None	-4	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL212614	79951	0	None	-4	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL385556	212354	0	None	-	1	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL3037885	210926	0	None	-1	2	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1016/s0960-894x(03)00114-8
	1324	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	16154396	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	16197727	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	44285019	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	57514683	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	91898441	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	CHEMBL441738	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	DB04931	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.0c00561
	CHEMBL3646880	212019	0	None	29	2	Human	9.5	pEC50	=	9.5	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	CHEMBL5090285	215253	0	None	-1	4	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL3358542	211569	0	None	2	3	Mouse	9.5	pEC50	=	9.5	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(C)=O)C(N)=O	10.1021/jm501027w
	1324	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	16154396	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	16197727	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	44285019	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	57514683	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	91898441	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	CHEMBL441738	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	DB04931	302	25	None	-9	9	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm010061n
	CHEMBL429236	213516	0	None	-15	4	Mouse	9.5	pEC50	=	9.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	44416057	81191	0	None	1	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL215833	81191	0	None	1	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	137637283	155980	0	None	2	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins	ChEMBL	984	15	12	10	-0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4061566	155980	0	None	2	3	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 40 mins	ChEMBL	984	15	12	10	-0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	122194229	123983	0	None	-14	5	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	CHEMBL3629347	123983	0	None	-14	5	Mouse	9.5	pEC50	=	9.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	1323	2688	55	None	-36	8	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
	92432	2688	55	None	-36	8	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
	CHEMBL430239	2688	55	None	-36	8	Human	9.5	pEC50	=	9.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
	CHEMBL415165	213176	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		None	10.1021/jm0501432
	56666386	63702	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801216	63702	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
	56676638	63693	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801146	63693	0	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL414965	213166	0	None	-8	5	Mouse	9.4	pEC50	=	9.4	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	11993702	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	5416	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	9272	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	CHEMBL3301624	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	DB11700	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
	1324	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	16154396	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	16197727	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	44285019	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	57514683	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	91898441	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	CHEMBL441738	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	DB04931	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.6b01707
	11993702	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	5416	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	9272	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	CHEMBL3301624	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	DB11700	3593	18	None	-2	4	Human	9.4	pEC50	=	9.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
	1324	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16154396	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16197727	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	44285019	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	57514683	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	91898441	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL441738	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	DB04931	302	25	None	-14	9	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL491870	214077	0	None	3	5	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	90643806	111746	0	None	-12	5	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	1324	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	16154396	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	16197727	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	44285019	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	57514683	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	91898441	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	CHEMBL441738	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	DB04931	302	25	None	-9	9	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00856
	CHEMBL3646891	212029	0	None	30	2	Human	9.4	pEC50	=	9.4	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	16172929	213001	15	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL412536	213001	15	None	-	1	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	6918780	63467	1	None	204	2	Human	9.4	pEC50	=	9.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	CHEMBL179836	63467	1	None	204	2	Human	9.4	pEC50	=	9.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	CHEMBL386081	212375	0	None	-23	4	Mouse	9.4	pEC50	=	9.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O	10.1021/jm010061n
	CHEMBL444219	213930	0	None	4	4	Mouse	9.4	pEC50	=	9.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	CHEMBL3287327	211310	0	None	-5	5	Human	9.4	pEC50	=	9.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL267794	210733	0	None	-13	4	Mouse	9.4	pEC50	=	9.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	CHEMBL405335	212556	0	None	-2	4	Mouse	9.4	pEC50	=	9.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	CHEMBL5090670	215277	0	None	3	4	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1324	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	16154396	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	16197727	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	44285019	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	57514683	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	91898441	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	CHEMBL441738	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	DB04931	302	25	None	-9	9	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
	CHEMBL2070244	209184	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	122194229	123983	0	None	-14	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.10.095
	CHEMBL3629347	123983	0	None	-14	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 2 hrs by cAMP alpha screen assay	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.10.095
	44416106	141446	0	None	4	3	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL384176	141446	0	None	4	3	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44448629	167463	0	None	3	4	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL429854	167463	0	None	3	4	Rat	9.3	pEC50	=	9.3	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL3646882	212021	0	None	35	2	Human	9.3	pEC50	=	9.3	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	1324	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL413912	213100	0	None	-7	3	Human	9.3	pEC50	=	9.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.07.046
	1324	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	16154396	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	16197727	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	44285019	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	57514683	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	91898441	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	CHEMBL441738	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	DB04931	302	25	None	-14	9	Human	9.3	pEC50	=	9.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
	CHEMBL5080784	214706	0	None	-2	4	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL264132	210606	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cncn2C)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	45487403	197435	0	None	-53	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	788	22	9	7	2.4	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569693	197435	0	None	-53	5	Mouse	9.3	pEC50	=	9.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	788	22	9	7	2.4	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CC1=CN=CC1)NC(=O)CCCc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL414718	213151	0	None	-	1	Human	9.3	pEC50	=	9.3	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
	127047475	139749	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	132991507	139749	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798421	139749	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL428801	213472	0	None	-21	5	Human	9.2	pEC50	=	9.2	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	118722939	116240	0	None	1	4	Mouse	9.2	pEC50	=	9.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358547	116240	0	None	1	4	Mouse	9.2	pEC50	=	9.2	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCCn2cc(nn2)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	10146211	64329	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL181162	64329	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	56669819	63691	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801144	63691	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
	49862748	15149	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209799	15149	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
	1323	2688	55	None	-36	8	Human	9.2	pEC50	=	9.2	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
	92432	2688	55	None	-36	8	Human	9.2	pEC50	=	9.2	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
	CHEMBL430239	2688	55	None	-36	8	Human	9.2	pEC50	=	9.2	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
	10146211	64329	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL181162	64329	0	None	61	3	Human	9.2	pEC50	=	9.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	11061068	31292	0	None	138	3	Human	9.2	pEC50	=	9.2	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
	CHEMBL140154	31292	0	None	138	3	Human	9.2	pEC50	=	9.2	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
	1338	3807	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL3646884	212022	0	None	39	2	Human	9.2	pEC50	=	9.2	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	CHEMBL412523	213000	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	129627786	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	1330	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16129617	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16129674	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133751	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133802	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16162116	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	3767	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	4516	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	60210072	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	6965	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL2103784	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	DB01284	280	32	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16132144	209279	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	16133793	209279	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	44273719	209279	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	CHEMBL214332	209279	36	None	-12	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm500064t
	127046235	139638	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3797690	139638	0	None	-2	5	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL428326	213438	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
	CHEMBL406842	212624	0	None	-6	5	Mouse	9.2	pEC50	=	9.2	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	56662904	63703	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801217	63703	0	None	-	1	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	90643803	111743	0	None	-1	5	Mouse	9.2	pEC50	=	9.2	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	111743	0	None	-1	5	Mouse	9.2	pEC50	=	9.2	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1338	3807	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	9.2	pEC50	=	9.2	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	1324	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	16154396	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	16197727	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	44285019	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	57514683	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	91898441	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	CHEMBL441738	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	DB04931	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960845e
	1324	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	16154396	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	16197727	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	44285019	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	57514683	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	91898441	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	CHEMBL441738	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	DB04931	302	25	None	-14	9	Human	9.1	pEC50	=	9.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm960840h
	56669820	63694	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
	CHEMBL1801147	63694	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
	CHEMBL410763	212838	0	None	-21	4	Mouse	9.1	pEC50	=	9.1	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	CHEMBL412494	212997	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	CHEMBL3601426	211826	0	None	17	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	56676632	63678	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801118	63678	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	25129453	171766	0	None	15	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
	CHEMBL446757	171766	0	None	15	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
	49862750	15152	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209801	15152	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL3358537	211568	0	None	-3	4	Mouse	9.1	pEC50	=	9.1	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C#CC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	1338	3807	43	None	-2	8	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL3646889	212027	0	None	31	2	Human	9.1	pEC50	=	9.1	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	118722940	116241	0	None	-1	4	Mouse	9.1	pEC50	=	9.1	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358548	116241	0	None	-1	4	Mouse	9.1	pEC50	=	9.1	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCCn2cc(nn2)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3646892	212030	0	None	25	2	Human	9.1	pEC50	=	9.1	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	56673302	63671	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801095	63671	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	1324	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16154396	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	16197727	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	44285019	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	57514683	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	91898441	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	CHEMBL441738	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	DB04931	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00251
	CHEMBL5077095	214479	0	None	-25	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	16746686	18156	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269575	18156	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	25133210	169457	0	None	44	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
	CHEMBL442829	169457	0	None	44	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
	25131478	169508	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
	CHEMBL443396	169508	0	None	-	1	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
	44569176	172545	0	None	48	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
	CHEMBL448410	172545	0	None	48	3	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
	44275650	94054	0	None	-2	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	953	15	12	10	-0.8	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL24892	94054	0	None	-2	4	Human	9.1	pEC50	=	9.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	953	15	12	10	-0.8	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1016/s0960-894x(03)00114-8
	1324	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	16154396	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	16197727	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	44285019	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	57514683	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	91898441	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	CHEMBL441738	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	DB04931	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse MC4R by alphascreen cAMP assayAgonist activity at mouse MC4R by alphascreen cAMP assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00641
	1324	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	16154396	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	16197727	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	44285019	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	57514683	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	91898441	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	CHEMBL441738	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	DB04931	302	25	None	-9	9	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
	10886436	119157	0	None	-1	5	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/acs.jmedchem.0c02041
	CHEMBL342954	119157	0	None	-1	5	Mouse	9.1	pEC50	=	9.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/acs.jmedchem.0c02041
	44448660	94973	0	None	4	4	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254589	94973	0	None	4	4	Rat	9.1	pEC50	=	9.1	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	56659466	63673	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801097	63673	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL427666	213364	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O	10.1021/jm0501432
	CHEMBL264190	210608	1	None	-30	8	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL264536	210627	5	None	-20	4	Mouse	9.0	pEC50	=	9.0	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm010061n
	127048118	173007	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4518266	173007	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL5087859	215123	0	None	-4	3	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	56683301	63697	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801150	63697	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
	1324	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	16154396	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	16197727	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	44285019	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	57514683	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	91898441	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	CHEMBL441738	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	DB04931	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00830-2
	1338	3807	43	None	-2	8	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	9938402	3807	43	None	-2	8	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	CHEMBL339053	3807	43	None	-2	8	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	56679968	63695	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801148	63695	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
	70688853	76924	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070248	76924	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	1324	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	11571540	135209	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL372201	135209	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	11593230	161230	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(C(N)=O)cc1	10.1016/j.bmcl.2005.08.083
	CHEMBL411817	161230	0	None	-	1	Human	9.0	pEC50	=	9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(C(N)=O)cc1	10.1016/j.bmcl.2005.08.083
	1324	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	16154396	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	16197727	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	44285019	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	57514683	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	91898441	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	CHEMBL441738	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	DB04931	302	25	None	-14	9	Human	9.0	pEC50	=	9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1016/s0960-894x(02)00459-6
	11851038	140335	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL5076315	214428	0	None	-3	4	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL3287059	211298	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL502093	214149	0	None	2	3	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	CHEMBL3799094	212268	0	None	-8	5	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	56673305	63683	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
	CHEMBL1801123	63683	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
	56676639	63696	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801149	63696	0	None	-	1	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
	49862736	15137	0	None	117	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209787	15137	0	None	117	2	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	1324	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	16154396	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	16197727	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	44285019	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	57514683	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	91898441	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	CHEMBL441738	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	DB04931	302	25	None	-9	9	Mouse	9.0	pEC50	=	9.0	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		None	10.1021/acsmedchemlett.9b00198
	46919520	15138	0	None	2	6	Rat	9.0	pEC50	=	9.0	Functional	Agonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209788	15138	0	None	2	6	Rat	9.0	pEC50	=	9.0	Functional	Agonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at rat melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	1324	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	1324	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	9.0	pEC50	=	9.0	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	168281421	190957	0	None	-10	3	Human	9.0	pEC50	=	9.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5185945	190957	0	None	-10	3	Human	9.0	pEC50	=	9.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	11158573	71119	0	None	-2	4	Mouse	8.9	pEC50	=	8.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	783	25	9	7	2.1	CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL195439	71119	0	None	-2	4	Mouse	8.9	pEC50	=	8.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	783	25	9	7	2.1	CCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	127047853	139993	0	None	-4	5	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3799955	139993	0	None	-4	5	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	56676614	63704	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801218	63704	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
	25129107	173777	0	None	36	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
	CHEMBL453734	173777	0	None	36	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
	1324	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	1338	3807	43	None	-2	8	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL5077144	214485	0	None	-13	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL5090946	215285	0	None	-4	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL322610	211234	0	None	-2	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL5091236	215299	0	None	-48	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44408287	75386	0	None	162	4	Human	8.9	pEC50	=	8.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	CHEMBL203911	75386	0	None	162	4	Human	8.9	pEC50	=	8.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	56659467	63686	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
	CHEMBL1801126	63686	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
	25133556	188849	0	None	7	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
	CHEMBL506762	188849	0	None	7	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
	168276507	190265	0	None	-15	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5175487	190265	0	None	-15	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	168289457	191380	0	None	-7	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5192329	191380	0	None	-7	4	Human	8.9	pEC50	=	8.9	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	137638778	156758	0	None	11	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4070639	156758	0	None	11	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	137633806	156481	0	None	10	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	CHEMBL4067491	156481	0	None	10	3	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	56662925	63676	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801116	63676	0	None	-	1	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL503229	214163	0	None	-1	4	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
	134466953	156658	0	None	-4	4	Mouse	8.9	pEC50	=	8.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1153	14	13	12	-1.3	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4069451	156658	0	None	-4	4	Mouse	8.9	pEC50	=	8.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1153	14	13	12	-1.3	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	1324	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	8.9	pEC50	=	8.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44310344	97329	0	None	-13	4	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	77231883	97329	0	None	-13	4	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	CHEMBL269274	97329	0	None	-13	4	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	CHEMBL443071	213920	0	None	-1	4	Human	8.9	pEC50	=	8.9	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	CHEMBL410404	212819	0	None	-11	5	Mouse	8.9	pEC50	=	8.9	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	10408	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	5329	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	9941379	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	CHEMBL2070241	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	DB11653	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
	10408	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	5329	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	9941379	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	CHEMBL2070241	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	DB11653	720	28	None	-1	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
	1338	3807	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	9938402	3807	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	CHEMBL339053	3807	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	CHEMBL3358533	211567	0	None	-3	4	Mouse	8.8	pEC50	=	8.8	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C#CC[C@H](NC(=O)[C@H](CCCC)NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	49862745	15146	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
	CHEMBL1209796	15146	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
	90643803	111743	0	None	-3	5	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	111743	0	None	-3	5	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	1338	3807	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL5087814	215119	0	None	-4	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	16132144	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	16133793	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	44273719	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0490843
	44415920	80371	0	None	2	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL214410	80371	0	None	2	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44416060	81318	0	None	66	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL215895	81318	0	None	66	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44415912	139226	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL378837	139226	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	56683299	63689	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801142	63689	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	134463477	159252	0	None	-5	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	977	11	12	11	-1.9	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4099127	159252	0	None	-5	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	977	11	12	11	-1.9	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	101670969	168896	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	16131138	168896	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	44349184	168896	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	53310908	168896	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	91898438	168896	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	CHEMBL438402	168896	23	None	-2	4	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	1623	49	22	22	-4.3	CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1021/acs.jmedchem.0c02041
	118722935	116236	0	None	1	4	Mouse	8.8	pEC50	=	8.8	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	CHEMBL3358543	116236	0	None	1	4	Mouse	8.8	pEC50	=	8.8	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1048	17	13	13	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm501027w
	42630327	155871	0	None	-6	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
	CHEMBL4060381	155871	0	None	-6	4	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
	16007263	79796	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL211975	79796	0	None	23	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	56683300	63690	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801143	63690	0	None	-	1	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	25129109	188702	0	None	29	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
	CHEMBL504349	188702	0	None	29	3	Human	8.8	pEC50	=	8.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
	16132144	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	16133793	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	44273719	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.8	pEC50	=	8.8	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.5b00053
	168293710	192166	0	None	-19	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5203986	192166	0	None	-19	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	168289404	191312	0	None	-39	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5191309	191312	0	None	-39	4	Human	8.8	pEC50	=	8.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	137635422	155910	0	None	30	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060816	155910	0	None	30	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL264190	210608	1	None	-30	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	24848934	78952	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113004	78952	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
	16132144	209279	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	16133793	209279	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	44273719	209279	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.7	pEC50	=	8.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0492756
	155531854	171648	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2286	54	25	25	-4.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4466007	171648	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	2286	54	25	25	-4.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	155563057	175298	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4573190	175298	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	56662927	63688	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
	CHEMBL1801141	63688	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
	CHEMBL3287069	211307	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)c(I)c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
	44456222	97925	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL272538	97925	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	49862376	15040	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209319	15040	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	25133208	171994	0	None	4	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
	CHEMBL447117	171994	0	None	4	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
	145977650	163834	0	None	-2	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4206406	163834	0	None	-2	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	1323	2688	55	None	-36	8	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	92432	2688	55	None	-36	8	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	CHEMBL430239	2688	55	None	-36	8	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	11845272	80358	0	None	9	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL214347	80358	0	None	9	3	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	44275265	161290	0	None	14	2	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3ccc(Br)cc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL412174	161290	0	None	14	2	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3ccc(Br)cc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	90643802	111742	0	None	-14	5	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287327	211310	0	None	-5	5	Human	8.0	pEC50	=	8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	11851038	140335	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44409257	140586	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	CHEMBL381357	140586	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	44409338	168744	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL437132	168744	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL412358	212986	0	None	-10	2	Human	8.0	pEC50	=	8	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)N=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	44441684	94131	0	None	28	3	Human	8.0	pEC50	=	8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL249321	94131	0	None	28	3	Human	8.0	pEC50	=	8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL264190	210608	1	None	-2	8	Mouse	8.0	pEC50	=	8.0	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	44448631	95070	0	None	1	4	Rat	8.0	pEC50	=	8.0	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL255286	95070	0	None	1	4	Rat	8.0	pEC50	=	8.0	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at rat MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL5081077	214717	0	None	-89	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	168295726	192405	0	None	-117	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5207936	192405	0	None	-117	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL589308	215799	0	None	-1	3	Mouse	8.0	pEC50	=	8.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCC(=O)N(CC(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)Cc1ccccc1	10.1016/j.bmc.2009.12.010
	44394659	66954	0	None	53	3	Human	8.0	pEC50	=	8.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	754	19	9	7	1.5	N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL186687	66954	0	None	53	3	Human	8.0	pEC50	=	8.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	754	19	9	7	1.5	N#CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11239907	133127	0	None	-18	4	Mouse	8.0	pEC50	=	8.0	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	854	30	9	7	4.1	CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL370261	133127	0	None	-18	4	Mouse	8.0	pEC50	=	8.0	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	854	30	9	7	4.1	CCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL264190	210608	1	None	-2	8	Mouse	8.0	pEC50	=	8.0	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	46228690	201492	0	None	-63	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL605115	201492	0	None	-63	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	137638218	156828	0	None	-2	4	Mouse	7.0	pEC50	=	7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	988	11	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4071283	156828	0	None	-2	4	Mouse	7.0	pEC50	=	7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	988	11	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	44373317	119658	0	None	2	2	Human	7.0	pEC50	=	7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL346930	119658	0	None	2	2	Human	7.0	pEC50	=	7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	16157270	212553	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	CHEMBL405282	212553	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	16157270	212553	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	CHEMBL405282	212553	14	None	-162	7	Human	7.0	pEC50	=	7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	71459896	78539	0	None	6	2	Human	6.0	pEC50	=	6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2112064	78539	0	None	6	2	Human	6.0	pEC50	=	6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	44442998	93606	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL246631	93606	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	44443016	94088	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
	CHEMBL249064	94088	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
	CHEMBL3600921	211824	0	None	-7	4	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	11706338	201707	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237150	201707	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237166	201707	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL606399	201707	0	None	-33	2	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	145966364	164120	0	None	-131	3	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4209913	164120	0	None	-131	3	Human	6.0	pEC50	=	6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL320157	211226	0	None	-1	4	Mouse	6.0	pEC50	=	6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	11851038	140335	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44349170	116823	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	650	9	4	5	4.8	O=C(NCc1ccccc1)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL337941	116823	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	650	9	4	5	4.8	O=C(NCc1ccccc1)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44348844	118203	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	4.0	CCC(C)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL340908	118203	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	4.0	CCC(C)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL381739	212292	0	None	-8	3	Human	5.0	pEC50	=	5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0510326
	44305763	203086	0	None	-5	4	Mouse	4.0	pEC50	=	4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	3.1	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	CHEMBL63850	203086	0	None	-5	4	Mouse	4.0	pEC50	=	4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	3.1	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCC(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	164612768	184719	0	None	-165	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	591	10	3	3	6.3	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4850501	184719	0	None	-165	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	591	10	3	3	6.3	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	164613353	184775	0	None	-	1	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	539	13	4	4	4.0	CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O	10.1021/acs.jmedchem.0c02041
	CHEMBL4851292	184775	0	None	-	1	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	539	13	4	4	4.0	CC(C)CCCN1C(=N)N([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C[C@H]1[C@@H](C)O	10.1021/acs.jmedchem.0c02041
	164613550	185129	0	None	-177	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	606	11	3	3	6.7	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4856539	185129	0	None	-177	3	Mouse	4.0	pEC50	=	4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	606	11	3	3	6.7	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	45487298	197342	0	None	-12	4	Mouse	5.0	pEC50	=	5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	657	17	8	8	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568965	197342	0	None	-12	4	Mouse	5.0	pEC50	=	5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	657	17	8	8	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	49862663	15122	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209705	15122	0	None	-	1	Human	6.0	pEC50	=	6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	44413576	78156	0	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	725	10	10	7	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL210399	78156	0	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	725	10	10	7	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL5091245	215300	0	None	-5	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	46228814	199376	0	None	-2	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	617	10	2	6	4.9	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3cc[nH]n3)(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL590955	199376	0	None	-2	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	617	10	2	6	4.9	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3cc[nH]n3)(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	137646617	157544	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4080223	157544	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44433423	88724	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL236110	88724	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	44433423	88724	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL236110	88724	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	46885368	7956	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1090484	7956	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	44275312	141407	0	None	70	2	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL384036	141407	0	None	70	2	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44394627	124081	0	None	7	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	20	8	6	2.1	CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL363272	124081	0	None	7	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	20	8	6	2.1	CCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	46228726	200491	0	None	-3	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598643	200491	0	None	-3	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	137646617	157544	0	None	-2	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4080223	157544	0	None	-2	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	46202892	7756	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	538	3	1	3	5.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1	10.1021/jm9017866
	CHEMBL1089107	7756	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	538	3	1	3	5.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1	10.1021/jm9017866
	CHEMBL1204062	7756	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	538	3	1	3	5.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C(F)(F)F)cc1	10.1021/jm9017866
	CHEMBL438596	213781	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44413969	80230	0	None	-24	3	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL213752	80230	0	None	-24	3	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	44310258	159418	0	None	-4	3	Mouse	5.0	pEC50	=	5.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932908	159418	0	None	-4	3	Mouse	5.0	pEC50	=	5.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL410091	159418	0	None	-4	3	Mouse	5.0	pEC50	=	5.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	44413968	80229	0	None	-57	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL213751	80229	0	None	-57	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL444493	213933	0	None	37	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL438596	213781	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44405911	140507	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	994	20	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)C1(NC(=O)Cc2ccccc2)CCc2c(Br)cccc2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL381007	140507	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	994	20	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)C1(NC(=O)Cc2ccccc2)CCc2c(Br)cccc2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	1337	3424	6	None	3	5	Human	8.0	pEC50	=	8.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	3424	6	None	3	5	Human	8.0	pEC50	=	8.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	3424	6	None	3	5	Human	8.0	pEC50	=	8.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	9808720	64222	0	None	3	2	Human	8.0	pEC50	=	8.0	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180892	64222	0	None	3	2	Human	8.0	pEC50	=	8.0	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
	6918813	131371	3	None	77	4	Human	8.0	pEC50	=	8.0	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL368876	131371	3	None	77	4	Human	8.0	pEC50	=	8.0	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL91957	215905	0	None	3	3	Human	8.0	pEC50	=	8.0	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	168278271	191115	0	None	-23	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5187932	191115	0	None	-23	4	Human	8.0	pEC50	=	8.0	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	137656521	159744	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4104927	159744	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44322895	163370	0	None	-5	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL419307	163370	0	None	-5	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44442954	94299	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL250495	94299	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	24848995	117947	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	CHEMBL340355	117947	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	145973975	164657	0	None	-16	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4216654	164657	0	None	-16	4	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643846	111768	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287353	111768	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	90643850	111771	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287357	111771	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44405802	72860	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200270	72860	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44349055	16466	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	613	9	2	8	3.1	COc1ccc(Cn2cncn2)c(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c1	10.1016/s0960-894x(03)00796-0
	CHEMBL123426	16466	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	613	9	2	8	3.1	COc1ccc(Cn2cncn2)c(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c1	10.1016/s0960-894x(03)00796-0
	11295737	120213	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL352063	120213	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	24848995	117947	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL340355	117947	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	70695694	78414	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2111251	78414	0	None	-1	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44397652	123634	0	None	14	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL361883	123634	0	None	14	2	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397461	126227	0	None	16	3	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365005	126227	0	None	16	3	Human	7.0	pEC50	=	7.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44448661	94999	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254792	94999	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44442931	150390	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL395355	150390	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44443027	155020	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL401488	155020	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44433384	154710	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL399801	154710	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	44433384	154710	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL399801	154710	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL3287356	211315	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	137645898	158018	0	None	-27	2	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	797	10	9	8	-1.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4085584	158018	0	None	-27	2	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	797	10	9	8	-1.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	155558348	175036	0	None	-61	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4567480	175036	0	None	-61	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155566298	175793	0	None	-85	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4584189	175793	0	None	-85	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL343094	211697	0	None	-6	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	44349006	114452	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	622	8	3	6	4.1	O=C(Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)c1cccnc1	10.1016/s0960-894x(03)00796-0
	CHEMBL333368	114452	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	622	8	3	6	4.1	O=C(Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)c1cccnc1	10.1016/s0960-894x(03)00796-0
	44397534	67268	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188142	67268	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397698	126201	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL364992	126201	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	1337	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	1337	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	1337	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	3424	6	None	3	5	Human	5.0	pEC50	=	5.0	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	46885561	7812	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cnccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089487	7812	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cnccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44441646	154088	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL398487	154088	0	None	10	3	Human	7.0	pEC50	=	7.0	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	122184912	122558	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601430	122558	0	None	-2	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	46203214	7861	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	3	1	5	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1	10.1021/jm9017866
	CHEMBL1089831	7861	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	3	1	5	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1	10.1021/jm9017866
	CHEMBL1204064	7861	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	3	1	5	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cncnc1	10.1021/jm9017866
	CHEMBL430843	213621	0	None	-3	3	Mouse	5.0	pEC50	=	5.0	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CCc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	16038121	106704	0	None	-8	2	Human	6.0	pEC50	=	6.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	697	10	10	7	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL3143817	106704	0	None	-8	2	Human	6.0	pEC50	=	6.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	697	10	10	7	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	46885674	7959	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	3	1	3	4.3	CC(C)(C)N1C[C@@H](C(=O)N2CCC(O)(c3ccccc3)CC2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1090487	7959	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	3	1	3	4.3	CC(C)(C)N1C[C@@H](C(=O)N2CCC(O)(c3ccccc3)CC2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	137656033	158643	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4092477	158643	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL65339	215860	0	None	-1	3	Mouse	5.0	pEC50	=	5.0	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	90643825	111749	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	923	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287331	111749	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	923	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44394657	127464	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	745	19	10	7	0.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL366040	127464	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	745	19	10	7	0.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	137647538	157962	0	None	-891	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4084765	157962	0	None	-891	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137638725	156979	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4073016	156979	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	90643844	111767	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287351	111767	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44372942	119757	0	None	-6	2	Human	5.9	pEC50	=	5.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	786	22	11	9	-1.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL347864	119757	0	None	-6	2	Human	5.9	pEC50	=	5.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	786	22	11	9	-1.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	45487417	197044	0	None	-27	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	CHEMBL567233	197044	0	None	-27	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C/C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	46885559	7810	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cncnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089484	7810	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cncnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	73347133	89472	0	None	-7	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371903	89472	0	None	-7	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	44416122	80128	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL213284	80128	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	56679964	63672	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801096	63672	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	25129105	177019	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
	CHEMBL463047	177019	0	None	12	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
	168273822	190570	0	None	-7	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5180152	190570	0	None	-7	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	11328898	7960	22	None	85	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1090488	7960	22	None	85	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1204059	7960	22	None	85	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	122179552	121487	0	None	-2	4	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12	10.1021/acsmedchemlett.5b00053
	CHEMBL3582446	121487	0	None	-2	4	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(N)=O)Cc1c[nH]c2ccccc12	10.1021/acsmedchemlett.5b00053
	1338	3807	43	None	-2	8	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL438596	213781	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	CHEMBL184870	209051	0	None	3	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		C=CCNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11786860	66334	1	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185035	66334	1	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	71454491	78953	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113006	78953	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	44441642	154405	0	None	75	3	Human	7.9	pEC50	=	7.9	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL398816	154405	0	None	75	3	Human	7.9	pEC50	=	7.9	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	162670951	182838	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791306	182838	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	137644225	158436	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4090425	158436	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL501679	214143	0	None	-1	3	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44277299	169432	0	None	8	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	864	23	9	8	1.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OCC)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL442537	169432	0	None	8	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	864	23	9	8	1.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OCC)C1	10.1016/s0960-894x(02)00830-2
	145976863	163758	0	None	-6	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	879	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4205548	163758	0	None	-6	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	879	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643838	111760	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287345	111760	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	1324	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	16154396	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	16197727	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	44285019	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	57514683	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	91898441	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	CHEMBL441738	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	DB04931	302	25	None	-9	9	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00318-4
	44397655	67307	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188360	67307	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	10168556	63873	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	CHEMBL180366	63873	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	137641398	158316	0	None	-162	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4089162	158316	0	None	-162	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44448479	155371	0	None	9	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL403420	155371	0	None	9	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	44442977	93814	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL247636	93814	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44443020	94089	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL249065	94089	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL264190	210608	1	None	-30	8	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	71456245	78976	0	None	2	4	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113039	78976	0	None	2	4	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44394694	66312	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	819	21	9	6	3.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL184895	66312	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	819	21	9	6	3.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL50056	214119	2	None	-117	7	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	44394580	122148	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	19	8	6	2.0	CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL359701	122148	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	757	19	8	6	2.0	CC(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	46944097	71918	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	441	6	1	5	5.3	COc1ccc(-c2cc(NC=O)c3ncc(-c4cccc(C(F)(F)F)c4)n3c2)cc1OC	nan
	CHEMBL1971975	71918	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	441	6	1	5	5.3	COc1ccc(-c2cc(NC=O)c3ncc(-c4cccc(C(F)(F)F)c4)n3c2)cc1OC	nan
	CHEMBL3287059	211298	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	137644225	158436	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4090425	158436	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1083	22	13	16	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	45487296	197325	0	None	-10	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	635	18	8	7	0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568836	197325	0	None	-10	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	635	18	8	7	0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccc(F)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL3287061	211300	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	46228764	200224	0	None	-35	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL596804	200224	0	None	-35	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	46885816	7906	0	None	28	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1090161	7906	0	None	28	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL2323800	209526	0	None	-79	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)[C@]23CCCN2C(=O)[C@@H](CSCC3=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	45487411	197045	0	None	-46	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL567240	197045	0	None	-46	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(O)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44278193	168437	0	None	22	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	862	22	9	7	2.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2C(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL434966	168437	0	None	22	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	862	22	9	7	2.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2C(C)C)C1	10.1016/s0960-894x(02)00830-2
	9808801	60809	0	None	29	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761871	60809	0	None	29	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
	10077258	15031	0	None	15	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209253	15031	0	None	15	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	118735100	118800	0	None	26	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421677	118800	0	None	26	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	162670951	182838	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791306	182838	0	None	4	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL3287329	211311	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287329	211311	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL451423	213968	0	None	1	4	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44373198	52166	0	None	7	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL158808	52166	0	None	7	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	10213106	72426	0	None	199	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198772	72426	0	None	199	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	71449119	78968	0	None	117	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL2113028	78968	0	None	117	2	Human	7.9	pEC50	=	7.9	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
	44323032	206604	0	None	-6	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL89004	206604	0	None	-6	3	Human	7.9	pEC50	=	7.9	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11308957	69393	0	None	-6	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	868	31	9	7	4.5	CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL193151	69393	0	None	-6	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	868	31	9	7	4.5	CCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	44448631	95070	0	None	-1	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL255286	95070	0	None	-1	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44400428	125677	0	None	-16	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	35	9	7	6.1	CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL364726	125677	0	None	-16	4	Mouse	7.9	pEC50	=	7.9	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	35	9	7	6.1	CCCCCCCCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL264190	210608	1	None	-2	8	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	44394585	66766	0	None	61	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	20	9	6	2.1	C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL185868	66766	0	None	61	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	20	9	6	2.1	C=CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL5077095	214479	0	None	-25	4	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL204310	209164	0	None	-64	4	Human	6.9	pEC50	=	6.9	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/jm0510326
	44278223	99135	0	None	5	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	878	23	9	8	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL281060	99135	0	None	5	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	878	23	9	8	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC(C)C)C1	10.1016/s0960-894x(02)00830-2
	44277301	100856	0	None	3	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29349	100856	0	None	3	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	145972289	164520	0	None	-45	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4214826	164520	0	None	-45	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643806	111746	0	None	-12	5	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	59149264	76802	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684624	76802	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929810	76802	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2069317	76802	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885862	8471	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	462	3	1	3	4.3	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	CHEMBL1093857	8471	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	462	3	1	3	4.3	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	CHEMBL2323793	209519	0	None	-17	4	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	137644449	158292	0	None	-3	3	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1016	12	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4088980	158292	0	None	-3	3	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1016	12	11	10	-0.7	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	44404528	72508	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL199037	72508	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44404528	72508	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL199037	72508	0	None	10	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	791	20	8	6	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	44448436	95602	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257770	95602	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44443015	94046	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL248862	94046	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44443031	154556	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL399112	154556	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL2323797	209523	0	None	-67	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@H]1CN2C(=O)CSC[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm301253y
	155555217	174337	0	None	-812	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4550976	174337	0	None	-812	4	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162667982	182415	0	None	-	1	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	776	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	CHEMBL4785727	182415	0	None	-	1	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	776	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	11364343	119924	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL349427	119924	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL184968	209052	0	None	7	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCC(=O)OC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	145980198	166686	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	692	17	7	6	2.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4282109	166686	0	None	1	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	692	17	7	6	2.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	164622453	186090	0	None	-2	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	12	3	3	6.2	CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2	10.1021/acs.jmedchem.0c02041
	CHEMBL4871577	186090	0	None	-2	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	12	3	3	6.2	CCC[C@@H]1CN([C@H](Cc2ccccc2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CC12CC3CC(CC(C3)C1)C2	10.1021/acs.jmedchem.0c02041
	162669632	182565	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787753	182565	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44310243	169187	0	None	-2	3	Mouse	4.9	pEC50	=	4.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932909	169187	0	None	-2	3	Mouse	4.9	pEC50	=	4.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL440633	169187	0	None	-2	3	Mouse	4.9	pEC50	=	4.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	44394734	64557	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	791	19	9	6	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL181494	64557	0	None	4	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	791	19	9	6	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	162669632	182565	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787753	182565	0	None	-1	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL434357	213652	0	None	5	3	Human	6.9	pEC50	=	6.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		COP(=O)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC	10.1016/j.bmcl.2004.07.046
	46232220	201054	0	None	-3	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602652	201054	0	None	-3	3	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	45487407	196968	0	None	-8	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL566545	196968	0	None	-8	3	Mouse	4.9	pEC50	=	4.9	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccccc1/C=C/C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	122184636	122435	0	None	-7	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600917	122435	0	None	-7	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	44393888	127082	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL365636	127082	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44408253	140344	0	None	54	4	Human	7.9	pEC50	=	7.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
	CHEMBL380727	140344	0	None	54	4	Human	7.9	pEC50	=	7.9	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
	52940633	18151	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269570	18151	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
	11846669	80277	0	None	2	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	CHEMBL213956	80277	0	None	2	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	44413930	138648	0	None	6	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL377620	138648	0	None	6	3	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	90643805	111745	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	111745	0	None	1	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643802	111742	0	None	-14	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	10325955	165271	0	None	112	2	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL423101	165271	0	None	112	2	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	11157584	168244	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL433710	168244	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44394730	132487	0	None	42	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	21	10	7	0.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL369770	132487	0	None	42	3	Human	7.9	pEC50	=	7.9	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	21	10	7	0.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11181928	166157	0	None	-4	4	Mouse	7.8	pEC50	=	7.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	797	26	9	7	2.5	CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL426282	166157	0	None	-4	4	Mouse	7.8	pEC50	=	7.8	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	797	26	9	7	2.5	CCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL3799094	212268	0	None	-12	5	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	44394660	67054	0	None	41	3	Human	7.8	pEC50	=	7.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	20	9	7	0.2	NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL187167	67054	0	None	41	3	Human	7.8	pEC50	=	7.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	772	20	9	7	0.2	NC(=O)CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44322958	107012	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL315356	107012	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL3350396	211479	0	None	-60	4	Human	7.8	pEC50	=	7.8	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	44415972	79883	0	None	141	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
	CHEMBL212332	79883	0	None	141	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
	155556954	174548	0	None	-467	4	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4556149	174548	0	None	-467	4	Mouse	6.9	pEC50	=	6.9	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	11262020	120267	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL352457	120267	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	73351850	89519	0	None	1	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2373212	89519	0	None	1	2	Human	6.9	pEC50	=	6.9	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44433475	148889	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	CHEMBL394160	148889	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	CHEMBL502300	214152	0	None	-27	4	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	71459937	78975	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113038	78975	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44409206	140184	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL380437	140184	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL309213	211015	0	None	1	2	Human	5.9	pEC50	=	5.9	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	11214733	120296	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL352677	120296	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	122184914	122559	0	None	-51	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601432	122559	0	None	-51	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL359765	211807	0	None	-1	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44393822	124043	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL363074	124043	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	46203216	8476	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1093889	8476	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204067	8476	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	137658158	159717	0	None	-10	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4104465	159717	0	None	-10	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487406	196894	0	None	-12	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.3	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL566150	196894	0	None	-12	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.3	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	44408388	140323	0	None	36	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL380635	140323	0	None	36	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	49862376	15040	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209319	15040	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
	44275192	168882	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL438286	168882	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	90643806	111746	0	None	-12	5	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	59149255	76928	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70693082	76928	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929809	76928	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070252	76928	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885480	7754	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089103	7754	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	46885621	7955	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	CHEMBL1090473	7955	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	CHEMBL1204057	7955	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	90643815	111719	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287066	111719	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	90643843	111766	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287350	111766	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287352	211314	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44405879	141234	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	946	20	9	7	3.8	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL382930	141234	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	946	20	9	7	3.8	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	44405794	161846	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	975	21	10	7	4.0	CCCCNC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL414670	161846	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	975	21	10	7	4.0	CCCCNC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	10030530	17599	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL125819	17599	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2004.06.059
	44393864	66196	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL184405	66196	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	10030530	17599	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125819	17599	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44413536	139929	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL379959	139929	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	145971389	164633	0	None	-15	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4216242	164633	0	None	-15	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	44457043	97612	0	None	-1	5	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL270923	97612	0	None	-1	5	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	137654884	158597	0	None	-3	3	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	840	9	10	9	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4092082	158597	0	None	-3	3	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	840	9	10	9	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	155542040	173078	0	None	-758	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4519837	173078	0	None	-758	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	44394584	96570	0	None	5	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	6	2.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL263047	96570	0	None	5	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	6	2.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11387898	56048	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL162493	56048	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	11237928	164871	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL422027	164871	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44401313	12287	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184856	12287	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028956	12287	0	None	-1	2	Human	6.8	pEC50	=	6.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44397633	126380	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365051	126380	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44442997	93922	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL248205	93922	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL320157	211226	0	None	-1	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	44447818	95410	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL256956	95410	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	44441686	97244	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL268722	97244	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
	11592389	199392	0	None	-6	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	591	8	1	5	5.4	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(OC(F)(F)F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591037	199392	0	None	-6	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	591	8	1	5	5.4	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(OC(F)(F)F)cc1	10.1016/j.bmc.2010.01.049
	45487404	197436	0	None	-3019	5	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	18	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569694	197436	0	None	-3019	5	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	18	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	122184575	122427	0	None	-2	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600836	122427	0	None	-2	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	122184909	122554	0	None	6	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601427	122554	0	None	6	4	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	44413879	138902	0	None	-50	3	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	CHEMBL378293	138902	0	None	-50	3	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	11851038	140335	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL433296	213636	0	None	-2	4	Mouse	6.8	pEC50	=	6.8	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	44394582	168374	0	None	2	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	21	8	6	2.5	CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL434544	168374	0	None	2	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	21	8	6	2.5	CCCCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44448698	94932	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254351	94932	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	90643842	111764	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287349	111764	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	16132144	209279	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44441648	154691	0	None	41	3	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL399715	154691	0	None	41	3	Human	6.8	pEC50	=	6.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	122184637	122436	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600918	122436	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	44413577	139526	0	None	-5	2	Human	5.8	pEC50	=	5.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL379531	139526	0	None	-5	2	Human	5.8	pEC50	=	5.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	46885325	8316	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	CHEMBL1092733	8316	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	44394626	65784	0	None	12	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	743	19	8	6	1.7	CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL183476	65784	0	None	12	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	743	19	8	6	1.7	CCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44310259	161700	0	None	1	2	Mouse	4.8	pEC50	=	4.8	Functional	Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932914	161700	0	None	1	2	Mouse	4.8	pEC50	=	4.8	Functional	Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL413465	161700	0	None	1	2	Mouse	4.8	pEC50	=	4.8	Functional	Effective concentration against mouse melanocortin MC4 receptor; Partial agonistEffective concentration against mouse melanocortin MC4 receptor; Partial agonist	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL413573	213075	0	None	-30	4	Human	7.8	pEC50	=	7.8	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
	44408252	140669	0	None	30	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL381503	140669	0	None	30	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	44408189	168879	0	None	32	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
	CHEMBL438259	168879	0	None	32	4	Human	7.8	pEC50	=	7.8	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
	10373417	100805	0	None	301	2	Human	7.8	pEC50	=	7.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29317	100805	0	None	301	2	Human	7.8	pEC50	=	7.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	44444495	154915	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL400932	154915	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	9867330	97841	0	None	14	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
	CHEMBL272099	97841	0	None	14	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cellsAgonist activity at human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
	44444495	154915	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL400932	154915	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	44444497	155012	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
	CHEMBL401465	155012	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
	9960253	116949	0	None	25	2	Human	7.8	pEC50	=	7.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL338594	116949	0	None	25	2	Human	7.8	pEC50	=	7.8	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	71456236	78890	0	None	-31	2	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112918	78890	0	None	-31	2	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	6918813	131371	3	None	77	4	Human	7.8	pEC50	=	7.8	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL368876	131371	3	None	77	4	Human	7.8	pEC50	=	7.8	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44413535	96705	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL264120	96705	0	None	4	2	Human	7.8	pEC50	=	7.8	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	44322977	111569	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL328117	111569	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	168271237	190488	0	None	-69	4	Human	7.8	pEC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5179081	190488	0	None	-69	4	Human	7.8	pEC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	155563222	175291	0	None	-524	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4572994	175291	0	None	-524	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155564058	175334	0	None	-794	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4574056	175334	0	None	-794	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	90643844	111767	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287351	111767	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	695	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44409140	141286	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL383256	141286	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	44405425	71860	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	CHEMBL197020	71860	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	44443033	93698	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL247010	93698	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
	CHEMBL264190	210608	1	None	-30	8	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	155556466	174416	0	None	-2238	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4552764	174416	0	None	-2238	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	44349151	18530	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	603	7	3	7	2.5	COC(=O)C(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL127461	18530	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	603	7	3	7	2.5	COC(=O)C(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44413842	138377	0	None	-3	3	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL377210	138377	0	None	-3	3	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44394010	125425	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL364577	125425	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	10188529	126781	0	None	19	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	CHEMBL365401	126781	0	None	19	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	46228846	199393	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	567	9	1	6	4.3	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591041	199393	0	None	8	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	567	9	1	6	4.3	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	25133903	170558	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
	CHEMBL445009	170558	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
	CHEMBL420581	213251	0	None	-27	2	Human	5.8	pEC50	=	5.8	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	44394093	127239	0	None	3	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	881	19	9	6	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365825	127239	0	None	3	3	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	881	19	9	6	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1c(F)c(F)c(F)c(F)c1F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44456138	95353	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL256686	95353	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	145989222	167280	0	None	1	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	676	17	7	6	2.2	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4293365	167280	0	None	1	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	676	17	7	6	2.2	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	44413932	137546	0	None	3	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
	CHEMBL375440	137546	0	None	3	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
	CHEMBL3287329	211311	0	None	1	5	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287064	211303	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL264190	210608	1	None	-2	8	Mouse	7.8	pEC50	=	7.8	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	49862742	14970	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1208802	14970	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL264190	210608	1	None	-2	8	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	137662147	159379	0	None	25	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4100598	159379	0	None	25	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	11555886	155634	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL404696	155634	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44443035	154417	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	CHEMBL398929	154417	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	44444493	155130	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL402058	155130	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
	CHEMBL432201	213633	0	None	6	5	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	57817730	76923	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684622	76923	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929805	76923	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070247	76923	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	137648053	157539	0	None	-10	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	934	12	11	10	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4080169	157539	0	None	-10	4	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	934	12	11	10	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	44349093	168522	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	633	8	2	7	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2c(Cn3cncn3)ccc3ccccc23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL435410	168522	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	633	8	2	7	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2c(Cn3cncn3)ccc3ccccc23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL439128	213825	0	None	-52	3	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	10141778	116719	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL337351	116719	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	46232228	201023	0	None	-5	3	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	8	8	1.0	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602299	201023	0	None	-5	3	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	8	8	1.0	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	45487413	197251	0	None	-14	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	616	15	10	7	-0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568409	197251	0	None	-14	4	Mouse	4.8	pEC50	=	4.8	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	616	15	10	7	-0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1cc2cc(O)ccc2[nH]1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44358915	13077	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL1190181	13077	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL540320	13077	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	137653925	158607	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4092141	158607	0	None	-4	4	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL263822	210590	0	None	-16	4	Human	6.8	pEC50	=	6.8	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
	44393886	66359	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185145	66359	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44275264	156381	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cccc(Br)c3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL406636	156381	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cccc(Br)c3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44441689	154418	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL398932	154418	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	15953838	67270	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL188146	67270	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL539306	67270	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	11635265	200486	0	None	-12	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	7	1	4	4.8	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598617	200486	0	None	-12	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	7	1	4	4.8	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	44335147	4592	0	None	-4	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	CHEMBL102688	4592	0	None	-4	4	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	CHEMBL275303	210821	0	None	4	4	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	11555886	155634	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
	CHEMBL404696	155634	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
	10483153	60811	0	None	53	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761873	60811	0	None	53	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	44416014	80015	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL212855	80015	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
	11555886	155634	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
	CHEMBL404696	155634	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
	145976444	163963	0	None	-6	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4207858	163963	0	None	-6	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	46885712	8071	0	None	63	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1091151	8071	0	None	63	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1204061	8071	0	None	63	4	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	46885417	8281	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092573	8281	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44456964	156690	0	None	1	4	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL406985	156690	0	None	1	4	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	16132144	209279	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	10145026	12269	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184727	12269	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028962	12269	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
	44393885	124387	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL363925	124387	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
	44390421	63906	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180544	63906	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
	44322923	206546	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL88630	206546	0	None	-2	3	Human	7.8	pEC50	=	7.8	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	127047913	139924	0	None	-19	5	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3799563	139924	0	None	-19	5	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL370254	212166	3	None	-6	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm0490843
	44394735	123315	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL361578	123315	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44278071	100444	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	704	20	9	7	-0.6	CCCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	CHEMBL29056	100444	0	None	1	2	Human	6.8	pEC50	=	6.8	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	704	20	9	7	-0.6	CCCC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	49862426	15061	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209383	15061	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
	15953838	67270	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188146	67270	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL539306	67270	0	None	18	3	Human	6.8	pEC50	=	6.8	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL415200	213179	0	None	-20	5	Mouse	6.8	pEC50	=	6.8	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(CCCN)CC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	1334	1501	7	None	-6	4	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		None	10.1021/jm030119t
	16133814	1501	7	None	-6	4	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		None	10.1021/jm030119t
	CHEMBL437050	1501	7	None	-6	4	Human	6.8	pEC50	=	6.8	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		None	10.1021/jm030119t
	44442995	93652	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL246837	93652	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	11364326	66686	0	None	-4	2	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	CHEMBL185455	66686	0	None	-4	2	Human	5.8	pEC50	=	5.8	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	168285101	191644	0	None	-85	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5195937	191644	0	None	-85	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	45487415	197439	0	None	-218	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569697	197439	0	None	-218	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	603	16	9	7	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(O)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44413913	138673	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	CHEMBL377779	138673	0	None	1	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	137643023	158310	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4089119	158310	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44394787	165988	0	None	4	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	821	21	9	7	2.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL425348	165988	0	None	4	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	821	21	9	7	2.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)COc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	90643819	111720	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287070	111720	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44441633	94530	0	None	18	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL251735	94530	0	None	18	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	44456137	155121	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
	CHEMBL402017	155121	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
	49862377	15041	0	None	13	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209320	15041	0	None	13	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	49862425	15060	0	None	74	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209382	15060	0	None	74	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	49862478	15075	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209458	15075	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	46885366	7851	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	5	1	3	4.4	CCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1089796	7851	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	5	1	3	4.4	CCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	11787684	70274	0	None	-6	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	811	27	9	7	2.9	CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL194217	70274	0	None	-6	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	811	27	9	7	2.9	CCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	16132144	209279	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	16133793	209279	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	44273719	209279	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	CHEMBL214332	209279	36	None	-8	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2009.07.025
	137631599	156526	0	None	-16	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4067967	156526	0	None	-16	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44443026	154802	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
	CHEMBL400263	154802	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
	90643802	111742	0	None	-14	5	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	102096778	58806	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	51351277	58806	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	53322400	58806	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	91932360	58806	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL1688111	58806	0	None	-10	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL2323794	209520	0	None	-21	3	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	44349173	116990	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/s0960-894x(03)00796-0
	CHEMBL338768	116990	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/s0960-894x(03)00796-0
	44393821	66712	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185583	66712	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL3349030	211405	0	None	-1	3	Human	6.7	pEC50	=	6.7	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	168285904	191670	0	None	-117	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5196407	191670	0	None	-117	4	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	44433380	88487	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	CHEMBL234992	88487	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
	11341045	66166	0	None	-4	2	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
	CHEMBL184275	66166	0	None	-4	2	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
	44349110	18551	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	559	7	3	5	3.4	CC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL127574	18551	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	559	7	3	5	3.4	CC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL264190	210608	1	None	-30	8	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	45487291	197373	0	None	-6	3	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569220	197373	0	None	-6	3	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C(F)=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44448480	95558	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257616	95558	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
	44409379	76522	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL206018	76522	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	137647538	157962	0	None	-891	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4084765	157962	0	None	-891	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL3287073	211309	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	49862662	15121	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209704	15121	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	44441639	94050	0	None	11	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL248893	94050	0	None	11	2	Human	6.7	pEC50	=	6.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	46232222	201055	0	None	-3	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	8	8	0.2	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602653	201055	0	None	-3	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	8	8	0.2	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	90643804	111744	0	None	-8	5	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-8	5	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	122184634	122433	0	None	-2	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600915	122433	0	None	-2	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	44456957	98038	0	None	-8	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	432	5	1	2	5.2	O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21	10.1021/jm701303z
	CHEMBL273044	98038	0	None	-8	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	432	5	1	2	5.2	O=C1NC(Cc2ccccc2)C(=O)N(Cc2ccccc2-c2ccccc2)c2ccccc21	10.1021/jm701303z
	10373417	100805	0	None	301	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29317	100805	0	None	301	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
	137638778	156758	0	None	11	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4070639	156758	0	None	11	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1053	18	14	15	-2.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44447251	154798	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at MC4RAgonist activity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
	CHEMBL400237	154798	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at MC4RAgonist activity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
	127047913	139924	0	None	-4	5	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3799563	139924	0	None	-4	5	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	44415918	141549	0	None	-1	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL384774	141549	0	None	-1	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	1323	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
	92432	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
	CHEMBL430239	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
	44569175	188822	0	None	12	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
	CHEMBL506272	188822	0	None	12	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
	73347133	89472	0	None	-7	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371903	89472	0	None	-7	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	44275656	159468	0	None	6	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	15	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL410148	159468	0	None	6	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	15	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2070242	209183	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	11753695	8393	7	None	3	8	Rat	8.7	pEC50	=	8.7	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093304	8393	7	None	3	8	Rat	8.7	pEC50	=	8.7	Functional	Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	1324	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44405858	72861	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	4.2	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200276	72861	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	4.2	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405833	133457	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	877	23	10	7	2.6	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL370665	133457	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	877	23	10	7	2.6	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405836	135208	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	882	21	9	7	2.5	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL372200	135208	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	882	21	9	7	2.5	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405860	136156	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	925	22	10	7	4.4	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL373259	136156	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	925	22	10	7	4.4	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	9919056	141069	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL382511	141069	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405793	158945	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(N)=O)c1	10.1016/j.bmcl.2005.08.083
	CHEMBL409588	158945	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	958	22	10	7	4.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCc1cccc(C(N)=O)c1	10.1016/j.bmcl.2005.08.083
	44405792	166110	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	940	23	10	7	4.1	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL425992	166110	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	940	23	10	7	4.1	CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405910	170456	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL444880	170456	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	910	22	9	7	3.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCc2cccc(C(N)=O)c2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200614	209108	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL		None	None	None		CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL434186	213651	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL		None	None	None		CCCCNC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	11273288	12960	0	None	61	3	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL1189370	12960	0	None	61	3	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL538567	12960	0	None	61	3	Human	8.7	pEC50	=	8.7	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	44404526	96492	0	None	346	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2cccc(OC)c2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL262470	96492	0	None	346	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2cccc(OC)c2)CC1	10.1016/j.bmcl.2005.08.012
	9919056	141069	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL382511	141069	0	None	1380	2	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL3644320	211960	0	None	30	2	Human	8.7	pEC50	=	8.7	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
	CHEMBL3646886	212024	0	None	39	2	Human	8.7	pEC50	=	8.7	Functional	cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.cAMP Assay: Accumulation of intracellular cAMP was examined as a measure of the ability of the peptides of the present invention to elicit a functional response in HEK-293 cells that express MC4-R. Confluent HEK-293 cells that express recombinant hMC4-R were detached from culture plates by incubation in enzyme-free cell dissociation buffer. Dispersed cells were suspended in Earle's Balanced Salt Solution containing 10 mM HEPES (pH 7.5), 1 mM MgCl2, 1 mM glutamine, 0.5% albumin and 0.3 mM 3-isobutyl-1-methyl-xanthine (IBMX), a phosphodiesterase inhibitor. The cells were plated in 96-well plates at a density of 0.5x105 cells per well and pre-incubated for 10 minutes. Cells were exposed for 15 minutes at 37° C. to peptides of the present invention dissolved in DMSO (final DMSO concentration of 1%) at a concentration range of 0.05-5000 nM in a total assay volume of 200 uL. NDP-α-MSH was used as the reference agonist. cAMP levels were determined by an HTRF cAMP cell-based assay system from Cisbio Bioassays utilizing cryptate-labeled anti-cAMP and d2-labeled cAMP, with plates read on a PerkinElmer Victor plate reader at 665 and 620 nM. Data analysis was performed by nonlinear regression analysis with Graph-Pad Prism software. The maximum efficacies of the test peptides of the present invention were compared to that achieved by the reference melanocortin agonist NDP-αMSH.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
	CHEMBL5083551	214869	0	None	-10	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1338	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
	9938402	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
	CHEMBL339053	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
	1338	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	9938402	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	CHEMBL339053	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
	1323	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL		None	None	None		None	10.1021/ml500436s
	92432	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL		None	None	None		None	10.1021/ml500436s
	CHEMBL430239	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL		None	None	None		None	10.1021/ml500436s
	44448629	167463	0	None	-3	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL429854	167463	0	None	-3	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	46911588	63668	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801092	63668	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	1323	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
	92432	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
	CHEMBL430239	2688	55	None	-36	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
	44358565	30026	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
	CHEMBL138901	30026	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
	1338	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	9938402	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL339053	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	1338	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	9938402	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL339053	3807	43	None	-2	8	Human	8.7	pEC50	=	8.7	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptorFunctional activity as concentration at 50% maximum cAMP accumulation in human Melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	118722929	116232	0	None	-2	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	CHEMBL3358538	116232	0	None	-2	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCN=[N+]=[N-])NC(=O)[C@H](CCCC)NC(C)=O)C(N)=O	10.1021/jm501027w
	10101361	155703	0	None	1	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL405174	155703	0	None	1	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL5078687	214580	0	None	-4	4	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	168271934	190085	0	None	-26	4	Human	8.7	pEC50	=	8.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5172738	190085	0	None	-26	4	Human	8.7	pEC50	=	8.7	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
	52943061	18148	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269568	18148	0	None	-	1	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	44416135	80184	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL213566	80184	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44416135	80184	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
	CHEMBL213566	80184	0	None	38	3	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
	16132144	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	16133793	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	44273719	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	CHEMBL214332	209279	36	None	-12	8	Human	8.7	pEC50	=	8.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
	118722925	116229	0	None	-3	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL3358534	116229	0	None	-3	4	Mouse	8.7	pEC50	=	8.7	Functional	Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assayActivity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay	ChEMBL	1052	34	13	11	1.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=[N+]=[N-])C(N)=O	10.1021/jm501027w
	CHEMBL264190	210608	1	None	-2	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	1323	2688	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
	92432	2688	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
	CHEMBL430239	2688	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
	137662147	159379	0	None	25	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4100598	159379	0	None	25	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1051	19	15	15	-3.0	C[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	52945472	18149	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269569	18149	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	56676635	63687	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801127	63687	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
	11845450	138469	0	None	-51	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL377465	138469	0	None	-51	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	44408286	140668	0	None	117	4	Human	8.6	pEC50	=	8.6	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	CHEMBL381501	140668	0	None	117	4	Human	8.6	pEC50	=	8.6	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	52941830	18155	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	CHEMBL1269574	18155	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
	90643802	111742	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2115441	209268	0	None	-8	4	Human	8.6	pEC50	=	8.6	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	10078903	68019	0	None	-7	4	Mouse	8.6	pEC50	=	8.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	769	24	9	7	1.8	CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL191303	68019	0	None	-7	4	Mouse	8.6	pEC50	=	8.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	769	24	9	7	1.8	CCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	16132144	209279	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	16133793	209279	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	44273719	209279	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm701303z
	CHEMBL5085972	215003	0	None	-1	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.1c00095
	CHEMBL5090670	215277	0	None	3	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	49862665	15124	0	None	128	2	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209707	15124	0	None	128	2	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	90643804	111744	0	None	-8	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-8	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	16132144	209279	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	90643841	111763	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287348	111763	0	None	-	1	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5087839	215120	0	None	2	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44418430	83255	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
	CHEMBL218748	83255	0	None	-1	3	Human	8.6	pEC50	=	8.6	Functional	Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulationActivity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
	25133209	173351	0	None	19	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
	CHEMBL452710	173351	0	None	19	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
	46919520	15138	0	None	-2	6	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209788	15138	0	None	-2	6	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	90643804	111744	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-2	5	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5094168	215479	0	None	-134	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	137637656	156238	0	None	40	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4064777	156238	0	None	40	3	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44448660	94973	0	None	-4	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL254589	94973	0	None	-4	4	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	1323	2688	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
	92432	2688	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
	CHEMBL430239	2688	55	None	-36	8	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
	90643806	111746	0	None	-12	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	8.6	pEC50	=	8.6	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL448536	213959	0	None	1	4	Mouse	8.6	pEC50	=	8.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C#N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	1323	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm070461w
	92432	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm070461w
	CHEMBL430239	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulationAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm070461w
	CHEMBL393075	212462	0	None	-7	4	Human	8.5	pEC50	=	8.5	Functional	Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2007.02.020
	168270124	189955	0	None	-20	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5170533	189955	0	None	-20	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	1323	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm0510326
	92432	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm0510326
	CHEMBL430239	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm0510326
	1323	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm060768f
	92432	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm060768f
	CHEMBL430239	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulationActivity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm060768f
	56683296	63679	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801119	63679	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
	1323	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		None	10.1021/jm801300c
	92432	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		None	10.1021/jm801300c
	CHEMBL430239	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		None	10.1021/jm801300c
	49862751	15153	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209802	15153	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
	1323	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
	92432	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
	CHEMBL430239	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
	90643804	111744	0	None	-8	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-8	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287327	211310	0	None	-5	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643803	111743	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	111743	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	16132144	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	16133793	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	44273719	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2015.09.046
	16132144	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44393824	122352	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	659	13	3	5	5.7	CCCC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ncc[nH]2)NC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL359976	122352	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	659	13	3	5	5.7	CCCC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ncc[nH]2)NC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2004.06.059
	1338	3807	43	None	2	8	Rat	8.5	pEC50	=	8.5	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	9938402	3807	43	None	2	8	Rat	8.5	pEC50	=	8.5	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL339053	3807	43	None	2	8	Rat	8.5	pEC50	=	8.5	Functional	Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)Functional activity as concentration at 50% maximum cAMP accumulation in rat Melanocortin-4 receptor (rMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
	CHEMBL410217	212808	0	None	2	3	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	44277696	101205	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	CHEMBL29582	101205	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
	44456027	155470	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL403967	155470	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
	44413938	138939	0	None	10	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL378446	138939	0	None	10	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL3287327	211310	0	None	-5	5	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2323795	209521	0	None	-39	4	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	90643826	111750	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287333	111750	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44277696	101205	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL29582	101205	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	44409339	74996	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL203252	74996	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
	CHEMBL78565	215880	0	None	-1	2	Human	7.7	pEC50	=	7.7	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	44394693	96598	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	805	20	9	6	2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL263234	96598	0	None	2	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	805	20	9	6	2.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44373177	119831	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL348511	119831	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44372933	119913	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL349298	119913	0	None	1	2	Human	7.7	pEC50	=	7.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44277696	101205	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
	CHEMBL29582	101205	0	None	1	4	Human	7.7	pEC50	=	7.7	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
	CHEMBL411400	212883	0	None	-141	5	Mouse	7.7	pEC50	=	7.7	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC1(C)C)C(N)=O	10.1021/jm030452x
	44323031	168078	0	None	-39	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL432565	168078	0	None	-39	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	71452720	78971	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL2113031	78971	0	None	34	3	Human	7.7	pEC50	=	7.7	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	44322812	112382	0	None	-5	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL329586	112382	0	None	-5	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11491374	67620	0	None	-21	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	840	29	9	7	3.7	CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL190366	67620	0	None	-21	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	840	29	9	7	3.7	CCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL501592	214141	0	None	-38	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	CHEMBL501642	214142	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL509582	215546	0	None	6	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	44405832	133584	0	None	14	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	909	21	8	7	2.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL371215	133584	0	None	14	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	909	21	8	7	2.7	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	11272336	57194	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164969	57194	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44397657	124123	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL363384	124123	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL438235	213759	0	None	-10	3	Human	6.7	pEC50	=	6.7	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C	10.1021/jm030119t
	CHEMBL446185	213944	0	None	-5	3	Human	5.7	pEC50	=	5.7	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0510326
	71459937	78975	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113038	78975	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44349226	116983	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL338747	116983	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	11845444	80067	0	None	-11	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL213026	80067	0	None	-11	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44413970	139015	0	None	-50	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL378571	139015	0	None	-50	3	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL2323792	209518	0	None	-2	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL438596	213781	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	118735103	118803	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421680	118803	0	None	-1	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	90643833	111756	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287340	111756	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL566764	215753	0	None	-2	2	Mouse	4.7	pEC50	=	4.7	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL		None	None	None		CC(=O)N/C(=C\c1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	90643819	111720	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287070	111720	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	688	13	6	6	1.8	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44393889	66347	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185094	66347	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44393877	122253	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL359777	122253	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL3287064	211303	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	46885524	7804	0	None	186	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1089462	7804	0	None	186	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1204054	7804	0	None	186	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL264190	210608	1	None	-2	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	16132144	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16132144	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL3287356	211315	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44394691	122903	0	None	15	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL360598	122903	0	None	15	3	Human	7.7	pEC50	=	7.7	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	11753667	57178	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164857	57178	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44441643	154800	0	None	43	2	Human	7.7	pEC50	=	7.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL400252	154800	0	None	43	2	Human	7.7	pEC50	=	7.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	44323034	206530	0	None	-1	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL88537	206530	0	None	-1	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11263053	68020	0	None	-29	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	33	9	7	5.3	CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL191304	68020	0	None	-29	4	Mouse	7.7	pEC50	=	7.7	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	896	33	9	7	5.3	CCCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL88185	215896	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44444508	155082	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL401853	155082	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL526334	215681	0	None	-1	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
	CHEMBL3287327	211310	0	None	-5	5	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2323529	209510	0	None	-2	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	11261324	58134	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL167780	58134	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44397569	122906	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL360602	122906	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL3600842	211819	0	None	-7	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL50056	214119	2	None	-117	7	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	44349008	114329	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	646	10	4	7	3.1	CCOC(=O)CNC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL333071	114329	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	646	10	4	7	3.1	CCOC(=O)CNC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	137659949	159132	0	None	-1	2	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3926	63	56	62	-18.1	CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CCCN2[C@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NC2=O	10.1021/acs.jmedchem.8b00251
	CHEMBL4097903	159132	0	None	-1	2	Human	4.7	pEC50	=	4.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3926	63	56	62	-18.1	CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H]2CCCN2[C@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NC2=O	10.1021/acs.jmedchem.8b00251
	52943061	18148	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269568	18148	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
	CHEMBL50056	214119	2	None	-117	7	Mouse	5.7	pEC50	=	5.7	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	16725558	155669	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL404905	155669	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
	90643847	111769	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287354	111769	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2369131	209593	0	None	-5	4	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	44441682	154648	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL399474	154648	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	168295131	192242	0	None	-14	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5205283	192242	0	None	-14	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL3600920	211823	0	None	-8	4	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	52918026	60808	0	None	63	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761870	60808	0	None	63	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
	11753695	8393	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4 receptorAgonist activity at mouse MC4 receptor	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1093304	8393	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4 receptorAgonist activity at mouse MC4 receptor	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	11753695	8393	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093304	8393	7	None	-10	8	Mouse	7.7	pEC50	=	7.7	Functional	Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	90643847	111769	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287354	111769	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44409104	76525	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	CHEMBL206033	76525	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
	44322957	206211	0	None	-3	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL86573	206211	0	None	-3	3	Human	7.7	pEC50	=	7.7	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL5075506	214379	0	None	-676	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL5091236	215299	0	None	-48	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44442972	153018	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397562	153018	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	145948912	167485	0	None	-8	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL	1170	17	14	11	0.7	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
	CHEMBL4299454	167485	0	None	-8	4	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMXAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX	ChEMBL	1170	17	14	11	0.7	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
	46885622	8459	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1093801	8459	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL2323785	209511	0	None	-35	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL500516	214117	0	None	1	4	Mouse	6.7	pEC50	=	6.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44405913	132736	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	21	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL369915	132736	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	21	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44349134	117323	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	12	2	6	4.4	CCC(CC)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL339708	117323	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	12	2	6	4.4	CCC(CC)N(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	90643833	111756	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287340	111756	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	46232225	201082	0	None	-6	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	8	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602852	201082	0	None	-6	3	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	8	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	90643828	111752	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287335	111752	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	90643834	111757	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287341	111757	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	118735102	118802	0	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	CHEMBL3421679	118802	0	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counterAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
	10348630	30196	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL139042	30196	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	45487295	197374	0	None	-13	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	18	8	7	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569221	197374	0	None	-13	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	18	8	7	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	137660671	159218	0	None	-812	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4098785	159218	0	None	-812	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137656489	159710	0	None	-1	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1125	13	13	12	-1.2	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4104402	159710	0	None	-1	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1125	13	13	12	-1.2	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL195468	209102	0	None	-7	4	Mouse	7.6	pEC50	=	7.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCCCCCCCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	44394583	122345	0	None	6	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	18	8	6	2.4	CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL359927	122345	0	None	6	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	771	18	8	6	2.4	CC(C)(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44442956	94348	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL250701	94348	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44397658	125426	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL364582	125426	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	155567399	175966	0	None	-501	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4588429	175966	0	None	-501	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL3287073	211309	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL432895	213635	4	None	-1	4	Mouse	5.6	pEC50	=	5.6	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	45487288	197356	0	None	-18	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	623	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569076	197356	0	None	-18	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	623	16	8	6	0.4	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(F)cc1F)C(N)=O	10.1016/j.bmcl.2009.07.025
	45487286	197341	0	None	-41	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	631	16	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568940	197341	0	None	-41	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	631	16	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	44358660	168559	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL435697	168559	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL544851	168559	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	44305790	102840	0	None	1	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	CHEMBL305559	102840	0	None	1	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	44305704	203337	0	None	1	4	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	CHEMBL64954	203337	0	None	1	4	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	407	10	5	3	2.4	NCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)NCc1ccccc1	10.1016/s0960-894x(03)00318-4
	44396986	67432	0	None	20	3	Human	6.6	pEC50	=	6.6	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL188966	67432	0	None	20	3	Human	6.6	pEC50	=	6.6	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	44278194	99370	0	None	8	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	848	22	9	7	1.9	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(CC)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL282533	99370	0	None	8	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	848	22	9	7	1.9	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(CC)cccc2C1	10.1016/s0960-894x(02)00830-2
	24873537	146061	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL391902	146061	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL2370964	209967	0	None	-74	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	90643830	111754	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287337	111754	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44349019	114437	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL333283	114437	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44322986	106097	0	None	-3	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL313377	106097	0	None	-3	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL2370964	209967	0	None	-74	4	Human	7.6	pEC50	=	7.6	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	16132144	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	16133793	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	44273719	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	CHEMBL214332	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	CHEMBL5087814	215119	0	None	-4	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	10098133	15015	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209191	15015	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL2323790	209516	0	None	-7	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	24882615	97492	0	None	-5	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	371	6	2	3	3.1	NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O	10.1021/jm701303z
	CHEMBL270270	97492	0	None	-5	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	371	6	2	3	3.1	NCCCCC1NC(=O)c2ccc(Cl)cc2N(Cc2ccccc2)C1=O	10.1021/jm701303z
	11157584	168244	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL433710	168244	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44358660	168559	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL435697	168559	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL544851	168559	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	122184577	122429	0	None	-19	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600838	122429	0	None	-19	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL105113	208466	0	None	-1	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	44349111	117486	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	10	2	6	4.2	CC(C)(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL339979	117486	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	679	10	2	6	4.2	CC(C)(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	44397651	66951	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL186675	66951	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	46885560	7811	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089485	7811	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44448628	155117	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL402009	155117	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL430489	213620	0	None	-2	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	137631599	156526	0	None	-16	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4067967	156526	0	None	-16	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	90643848	111770	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287355	111770	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	137660671	159218	0	None	-812	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4098785	159218	0	None	-812	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137658158	159717	0	None	-10	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4104465	159717	0	None	-10	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	16132144	209279	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	16133793	209279	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	44273719	209279	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	CHEMBL214332	209279	36	None	-8	8	Mouse	5.6	pEC50	=	5.6	Functional	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsCompound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00318-4
	44413880	77946	0	None	-10	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
	CHEMBL209587	77946	0	None	-10	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
	16132144	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	16133793	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	44273719	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	CHEMBL214332	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00830-2
	10257242	15030	0	None	39	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209252	15030	0	None	39	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	10077258	15031	0	None	15	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209253	15031	0	None	15	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	25132867	172498	0	None	15	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
	CHEMBL448337	172498	0	None	15	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
	CHEMBL2371888	210146	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(C)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	71452716	78893	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL2112920	78893	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL322610	211234	0	None	-2	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	16132144	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	16133793	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	44273719	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	CHEMBL214332	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(02)00459-6
	71452716	78893	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112920	78893	0	None	2	2	Human	7.6	pEC50	=	7.6	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL508501	214942	0	None	36	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL438596	213781	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	CHEMBL438596	213781	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	90643848	111770	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287355	111770	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44358630	28314	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL137452	28314	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL541866	28314	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL443590	213925	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	CHEMBL311175	211098	0	None	-2	2	Human	5.6	pEC50	=	5.6	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	11845630	139514	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL379490	139514	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44394009	124350	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL363684	124350	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	44413881	137593	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	CHEMBL375559	137593	0	None	4	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
	46885324	8210	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1092210	8210	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	432	3	2	3	3.4	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	45487287	197649	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	633	17	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL570903	197649	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	633	17	8	8	-0.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cccc2c1OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	46886010	7874	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1089892	7874	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	3	4.7	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	137649543	157320	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4077331	157320	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	155549760	173877	0	None	-66	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4539621	173877	0	None	-66	4	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	1338	3807	43	None	-2	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL2310901	209498	0	None	-4	4	Human	7.6	pEC50	=	7.6	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	CHEMBL5087859	215123	0	None	-4	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44322959	156075	0	None	-13	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL406276	156075	0	None	-13	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	11423083	96839	0	None	-26	4	Mouse	7.6	pEC50	=	7.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	882	32	9	7	4.9	CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL265236	96839	0	None	-26	4	Mouse	7.6	pEC50	=	7.6	Functional	In vitro agonist potency for Mouse Melanocortin 4 receptorIn vitro agonist potency for Mouse Melanocortin 4 receptor	ChEMBL	882	32	9	7	4.9	CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0490843
	CHEMBL3287327	211310	0	None	-5	5	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	155539948	172886	0	None	-131	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4515666	172886	0	None	-131	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL138771	208754	0	None	1	3	Mouse	6.6	pEC50	=	6.6	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N(CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1	10.1016/j.bmcl.2003.08.078
	44358705	96625	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL263461	96625	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	1334	1501	7	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	16133814	1501	7	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	CHEMBL437050	1501	7	None	-6	4	Human	6.6	pEC50	=	6.6	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm000211e
	49789765	67232	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	363	4	1	5	4.7	COc1cccc(-c2cnc3c(NC(C)=O)cc(-c4ccsc4)cn23)c1	nan
	CHEMBL1879413	67232	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	363	4	1	5	4.7	COc1cccc(-c2cnc3c(NC(C)=O)cc(-c4ccsc4)cn23)c1	nan
	CHEMBL3600841	211818	0	None	-1	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	11845276	80053	0	None	2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
	CHEMBL212976	80053	0	None	2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
	1334	1501	7	None	-6	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133814	1501	7	None	-6	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL437050	1501	7	None	-6	4	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	90643838	111760	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287345	111760	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	831	10	3	5	4.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44456304	155254	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	CHEMBL402787	155254	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	56676633	63681	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801121	63681	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
	16132144	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44394736	123316	0	None	25	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL361579	123316	0	None	25	3	Human	7.6	pEC50	=	7.6	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	797	19	9	7	2.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44390424	63927	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180635	63927	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	137660993	159447	0	None	-63	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4101216	159447	0	None	-63	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44433448	88484	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL234983	88484	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	44433448	88484	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL234983	88484	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	145966716	164305	0	None	-70	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4212209	164305	0	None	-70	4	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL2070254	209185	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	155567887	176048	0	None	1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	676	19	10	7	-1.1	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4590532	176048	0	None	1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	676	19	10	7	-1.1	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	164623811	185900	0	None	-1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	614	11	4	4	6.2	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4868636	185900	0	None	-1	4	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	614	11	4	4	6.2	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL438596	213781	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44391940	12250	0	None	21	2	Human	6.6	pEC50	=	6.6	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1184624	12250	0	None	21	2	Human	6.6	pEC50	=	6.6	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145456	12250	0	None	21	2	Human	6.6	pEC50	=	6.6	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44405366	71961	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	CHEMBL197327	71961	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	11375764	66689	0	None	-38	2	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	CHEMBL185469	66689	0	None	-38	2	Human	5.6	pEC50	=	5.6	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
	CHEMBL414778	213156	0	None	-478	4	Human	5.6	pEC50	=	5.6	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	90643850	111771	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287357	111771	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44359589	31479	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	685	20	4	7	1.4	CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1	10.1016/j.bmcl.2003.08.078
	CHEMBL140324	31479	0	None	-3	3	Mouse	4.6	pEC50	=	4.6	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	685	20	4	7	1.4	CC(=O)N(CCc1c[nH]cn1)CC(=O)N(CC(=O)N(CCCCN)CC(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O)Cc1ccccc1	10.1016/j.bmcl.2003.08.078
	51350911	58804	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53322399	58804	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932357	58804	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688109	58804	0	None	-5	3	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	11156852	65685	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL183434	65685	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44394078	161717	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL413556	161717	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	90643834	111757	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287341	111757	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	56669816	63677	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801117	63677	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
	25133907	176724	0	None	5	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	CHEMBL460138	176724	0	None	5	3	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	162672255	182871	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791788	182871	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	90643823	111721	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287074	111721	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	44323033	107152	0	None	-4	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL316259	107152	0	None	-4	3	Human	7.6	pEC50	=	7.6	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	162672255	182871	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4791788	182871	0	None	1	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL5077144	214485	0	None	-13	4	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44441645	94127	0	None	63	3	Human	7.5	pEC50	=	7.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL249277	94127	0	None	63	3	Human	7.5	pEC50	=	7.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	137637656	156238	0	None	40	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4064777	156238	0	None	40	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1045	20	14	15	-2.2	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	145988867	167103	0	None	-3	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	660	17	7	6	1.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4289983	167103	0	None	-3	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	660	17	7	6	1.7	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	133053557	163706	0	None	-15	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4204975	163706	0	None	-15	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643824	111748	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287330	111748	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643828	111752	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287335	111752	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44405378	140565	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	CHEMBL381197	140565	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
	44305956	102761	0	None	1	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	2.9	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	CHEMBL305132	102761	0	None	1	4	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	490	11	5	4	2.9	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NC1CCN(Cc2ccccc2)CC1	10.1016/s0960-894x(03)00318-4
	44441636	94012	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL248701	94012	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	11512024	200485	0	None	-5	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598616	200485	0	None	-5	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	46885326	8211	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	450	3	2	3	3.5	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	CHEMBL1092211	8211	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	450	3	2	3	3.5	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)c(F)c1	10.1021/jm9017866
	46228813	201449	0	None	-16	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	538	8	1	6	3.9	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL604911	201449	0	None	-16	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	538	8	1	6	3.9	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	49862378	15042	0	None	45	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209321	15042	0	None	45	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	11170774	158364	1	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assayAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assay	ChEMBL	1180	19	13	12	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)C(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4089689	158364	1	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assayAgonist activity at human MC4R expressed in CHO cells assessed as increase in IBMX-induced cAMP accumulation after 45 mins by [125I]cAMP flash plate assay	ChEMBL	1180	19	13	12	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)C(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	137656180	159028	0	None	-13	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1005	12	12	11	-2.0	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4096678	159028	0	None	-13	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	1005	12	12	11	-2.0	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL2096759	209208	0	None	-7	4	Human	7.5	pEC50	=	7.5	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	44391927	13991	0	None	57	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL1196971	13991	0	None	57	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL3216393	13991	0	None	57	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL187125	209055	0	None	30	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)Nc1ccco1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL89270	215899	0	None	1	3	Human	7.5	pEC50	=	7.5	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1016/s0960-894x(03)00552-3
	73353216	89476	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2372046	89476	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	11181804	128507	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	CHEMBL366706	128507	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
	CHEMBL2323789	209515	0	None	-147	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	73353216	89476	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	CHEMBL2372046	89476	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	11237444	127465	0	None	-5	2	Human	5.5	pEC50	=	5.5	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
	CHEMBL366042	127465	0	None	-5	2	Human	5.5	pEC50	=	5.5	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
	11845813	139804	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	CHEMBL379879	139804	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	11847312	79762	0	None	1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	CHEMBL211798	79762	0	None	1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
	CHEMBL3287338	211312	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	73353216	89476	0	None	5	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2372046	89476	0	None	5	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	806	20	9	7	0.9	CCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	90643802	111742	0	None	-14	5	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL275303	210821	0	None	4	4	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	25128749	178470	0	None	37	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
	CHEMBL466380	178470	0	None	37	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
	73348634	89471	0	None	1	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	10	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371902	89471	0	None	1	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	10	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	90643806	111746	0	None	-12	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44405681	71793	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	2.9	C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL196773	71793	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	21	9	7	2.9	C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(N)=O	10.1016/j.bmcl.2005.08.083
	44405826	141271	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	21	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL383143	141271	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	21	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C)C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405857	158947	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	944	21	10	7	4.9	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	CHEMBL409589	158947	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	944	21	10	7	4.9	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccccc1C(N)=O	10.1016/j.bmcl.2005.08.083
	44401522	12784	0	None	97	2	Human	8.5	pEC50	=	8.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1188041	12784	0	None	97	2	Human	8.5	pEC50	=	8.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL534928	12784	0	None	97	2	Human	8.5	pEC50	=	8.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44404522	72291	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	862	22	9	7	2.8	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198309	72291	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	862	22	9	7	2.8	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	168284256	190946	0	None	-64	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5185775	190946	0	None	-64	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	16132144	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	16133793	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	44273719	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.5	pEC50	=	8.5	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010061n
	137659790	159322	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL4099889	159322	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1323	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	92432	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL430239	2688	55	None	-36	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	49862749	15151	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209800	15151	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
	CHEMBL3287327	211310	0	None	-1	5	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5094215	215481	0	None	-15	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	137637026	155925	0	None	28	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060937	155925	0	None	28	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	11215553	8394	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093305	8394	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	145964017	164041	0	None	1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4208874	164041	0	None	1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	90643803	111743	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	111743	0	None	-3	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL438596	213781	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	44441641	94301	0	None	69	3	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL250508	94301	0	None	69	3	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	16172929	213001	15	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		None	10.1021/jm0501432
	CHEMBL412536	213001	15	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		None	10.1021/jm0501432
	11215553	8394	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1093305	8394	0	None	60	2	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	49862747	15148	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209798	15148	0	None	-	1	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL2371712	210109	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	CHEMBL413260	213059	0	None	5	2	Human	8.5	pEC50	=	8.5	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	CHEMBL5075712	214394	0	None	-102	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643805	111745	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	111745	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643808	111747	0	None	-14	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	16132144	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	16133793	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	44273719	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	CHEMBL214332	209279	36	None	-12	8	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
	CHEMBL501394	214137	0	None	2	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	46919520	15138	0	None	-3	6	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209788	15138	0	None	-3	6	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at mouse melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL5090285	215253	0	None	-1	4	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643805	111745	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	111745	0	None	1	5	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	168272660	190433	0	None	-28	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5178164	190433	0	None	-28	4	Human	8.5	pEC50	=	8.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	127047475	139749	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	132991507	139749	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3798421	139749	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3287338	211312	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3349030	211405	0	None	-1	3	Human	8.4	pEC50	=	8.4	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	1338	3807	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
	9938402	3807	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
	CHEMBL339053	3807	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
	44413914	139518	0	None	-12	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL379508	139518	0	None	-12	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	16132144	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	16133793	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	44273719	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acsmedchemlett.9b00198
	44456222	97925	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL272538	97925	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	11296600	122943	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	CHEMBL360716	122943	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as stimulation of cAMP production	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	56679956	63700	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801214	63700	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	49862746	15147	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209797	15147	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	90643802	111742	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	11296600	122943	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360716	122943	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL5091245	215300	0	None	-5	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44441644	154838	0	None	66	3	Human	8.4	pEC50	=	8.4	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL400456	154838	0	None	66	3	Human	8.4	pEC50	=	8.4	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL322610	211234	0	None	-2	4	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	46885711	8070	0	None	123	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	CHEMBL1091150	8070	0	None	123	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
	155543031	173181	0	None	-50	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4522298	173181	0	None	-50	4	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	44394692	66214	0	None	17	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL184466	66214	0	None	17	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	71459938	78981	0	None	4	4	Human	7.5	pEC50	=	7.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113043	78981	0	None	4	4	Human	7.5	pEC50	=	7.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	44393823	123974	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL362880	123974	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	44405450	72518	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL199061	72518	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL427205	213352	0	None	-21	3	Human	5.5	pEC50	=	5.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
	155565321	175576	0	None	-100	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4579448	175576	0	None	-100	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	168274920	190263	0	None	-102	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5175444	190263	0	None	-102	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL321870	211232	0	None	-5	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	51350799	58801	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53323763	58801	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932356	58801	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688105	58801	0	None	-7	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	44358698	30924	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL139803	30924	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	56676634	63684	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	CHEMBL1801124	63684	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	168272615	190387	0	None	-60	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5177494	190387	0	None	-60	4	Human	6.5	pEC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	137655905	158828	0	None	-74	4	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4094606	158828	0	None	-74	4	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	44444507	94173	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL249571	94173	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	25132524	176758	0	None	7	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	CHEMBL460349	176758	0	None	7	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
	44394690	124648	0	None	14	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL364119	124648	0	None	14	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	792	19	9	7	2.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44394658	168337	0	None	5	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	758	18	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL434329	168337	0	None	5	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	758	18	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	162672691	183201	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4795842	183201	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL5076315	214428	0	None	-3	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643837	111759	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287344	111759	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	155562237	175709	0	None	-1548	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4582276	175709	0	None	-1548	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	9852256	175367	0	None	-7	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	632	15	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4574756	175367	0	None	-7	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	632	15	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	45487300	197359	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	15	8	8	-0.6	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569086	197359	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	605	15	8	8	-0.6	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)c1ccc2c(c1)OCO2)C(N)=O	10.1016/j.bmcl.2009.07.025
	44413537	139547	0	None	-2	2	Human	5.5	pEC50	=	5.5	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL379627	139547	0	None	-2	2	Human	5.5	pEC50	=	5.5	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	46228845	199388	0	None	-39	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	9	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(Cc3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591026	199388	0	None	-39	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	9	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(Cc3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228848	199399	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	8	0	6	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3nn(C)c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591061	199399	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	551	8	0	6	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3nn(C)c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228849	199411	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	595	10	0	7	4.8	CCn1nc(CC2(OC)C(=O)N(CC(=O)N(c3ccc(OC)cc3)C(C)C)C=CN(c3ccccc3)C2=O)c2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL591123	199411	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	595	10	0	7	4.8	CCn1nc(CC2(OC)C(=O)N(CC(=O)N(c3ccc(OC)cc3)C(C)C)C=CN(c3ccccc3)C2=O)c2ccccc21	10.1016/j.bmc.2010.01.049
	46228847	199413	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	620	11	1	7	6.0	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(Oc1ccccc1)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL591132	199413	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	620	11	1	7	6.0	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(Oc1ccccc1)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	46228842	199416	0	None	-38	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	592	8	1	6	4.3	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(N2CCOCC2)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591194	199416	0	None	-38	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	592	8	1	6	4.3	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(N2CCOCC2)cc1	10.1016/j.bmc.2010.01.049
	46228844	199417	0	None	-26	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	587	10	1	7	4.3	COc1ccc(N(C(=O)CN2C=CN(Cc3cccs3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591195	199417	0	None	-26	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	587	10	1	7	4.3	COc1ccc(N(C(=O)CN2C=CN(Cc3cccs3)C(=O)C(Cc3n[nH]c4ccccc34)(OC)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228888	199487	0	None	-8	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	481	6	1	4	3.2	CC(C)N(C(=O)CN1C=CN(C)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL591717	199487	0	None	-8	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	481	6	1	4	3.2	CC(C)N(C(=O)CN1C=CN(C)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccc(F)cc1	10.1016/j.bmc.2010.01.049
	46228763	200186	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL596602	200186	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	46228659	200393	0	None	-20	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598010	200393	0	None	-20	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228850	200427	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	544	9	2	6	3.9	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(O)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598208	200427	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	544	9	2	6	3.9	O=C(CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)CP(=O)(O)Oc1ccccc1	10.1016/j.bmc.2010.01.049
	46228725	200457	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598442	200457	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)[C@@H](Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	46228841	200525	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	503	8	0	4	4.8	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3ccccc3)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598831	200525	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	503	8	0	4	4.8	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3ccccc3)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	46228843	201645	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	8	1	5	4.6	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL605970	201645	0	None	-1	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	543	8	1	5	4.6	COc1ccc(N(C(=O)CN2C=CN(C3CCCCC3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	11706338	201707	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237150	201707	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL1237166	201707	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL606399	201707	0	None	-33	2	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	523	7	2	5	4.2	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccc(O)cc1	10.1016/j.bmc.2010.01.049
	11846673	79994	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL212766	79994	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	137643385	158131	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4087072	158131	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	90643836	111758	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287343	111758	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	56666397	63674	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801098	63674	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	162672691	183201	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4795842	183201	0	None	4	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	46885415	8279	0	None	10	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092571	8279	0	None	10	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL432201	213633	0	None	6	5	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44444432	94404	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	CHEMBL250976	94404	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	44397356	66917	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL186557	66917	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44431512	145924	0	None	-87	4	Human	5.5	pEC50	=	5.5	Functional	Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
	CHEMBL391796	145924	0	None	-87	4	Human	5.5	pEC50	=	5.5	Functional	Effect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulationEffect on human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
	CHEMBL3287352	211314	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	51351024	58802	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53318435	58802	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932358	58802	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688106	58802	0	None	-13	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N2C[C@@H](Cc3ccccc3)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	11685018	200693	0	None	-204	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL599867	200693	0	None	-204	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	11627577	201191	0	None	-4	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL603468	201191	0	None	-4	2	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	507	7	1	4	4.5	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL438596	213781	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	CHEMBL80803	215885	0	None	-9	2	Human	5.5	pEC50	=	5.5	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	10123761	99493	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL283214	99493	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	44275121	96486	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Cl)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL262437	96486	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Cl)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11851038	140335	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	11636019	72360	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL198535	72360	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	49862739	15141	0	None	23	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209791	15141	0	None	23	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	44401585	13763	0	None	19	2	Human	6.5	pEC50	=	6.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL1195347	13763	0	None	19	2	Human	6.5	pEC50	=	6.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	CHEMBL554368	13763	0	None	19	2	Human	6.5	pEC50	=	6.5	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
	46232227	199170	0	None	-6	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL589517	199170	0	None	-6	3	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	137660993	159447	0	None	-63	4	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4101216	159447	0	None	-63	4	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	46228660	200394	0	None	-21	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598011	200394	0	None	-21	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)[C@H](Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	90643808	111747	0	None	-14	5	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271R mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	11341811	120124	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL351161	120124	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44393863	127553	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL366321	127553	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL439691	213848	0	None	-5	3	Human	7.5	pEC50	=	7.5	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	44391938	11746	0	None	20	2	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1181567	11746	0	None	20	2	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145455	11746	0	None	20	2	Human	7.5	pEC50	=	7.5	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44397220	167304	0	None	28	3	Human	7.5	pEC50	=	7.5	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	CHEMBL429387	167304	0	None	28	3	Human	7.5	pEC50	=	7.5	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
	CHEMBL438030	213744	0	None	-21	3	Human	7.5	pEC50	=	7.5	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	CHEMBL204864	209166	0	None	-12	4	Human	6.5	pEC50	=	6.5	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O	10.1021/jm0510326
	44455893	155638	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL404706	155638	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL409636	212773	0	None	-1	3	Human	6.5	pEC50	=	6.5	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm030119t
	44349228	18815	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL127861	18815	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44305770	202794	0	None	-1	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	448	9	5	4	2.2	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1	10.1016/s0960-894x(03)00318-4
	CHEMBL62228	202794	0	None	-1	4	Mouse	5.5	pEC50	=	5.5	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	448	9	5	4	2.2	NCCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NN1CCc2ccccc2C1	10.1016/s0960-894x(03)00318-4
	CHEMBL431242	213624	0	None	-1	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	46885713	7799	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C#N)cc1	10.1021/jm9017866
	CHEMBL1089442	7799	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(C#N)cc1	10.1021/jm9017866
	44278195	98806	0	None	35	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	834	21	9	7	1.6	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(C)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL27848	98806	0	None	35	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	834	21	9	7	1.6	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(C)cccc2C1	10.1016/s0960-894x(02)00830-2
	10123761	99493	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL283214	99493	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
	44275119	169020	0	None	37	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1033	15	11	10	1.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OCC)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL439361	169020	0	None	37	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1033	15	11	10	1.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OCC)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	10123761	99493	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL283214	99493	0	None	15	2	Human	7.5	pEC50	=	7.5	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL185869	209053	0	None	6	3	Human	7.5	pEC50	=	7.5	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCOC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL3600843	211820	0	None	-4	4	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	51350673	58800	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53317148	58800	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932362	58800	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688104	58800	0	None	-1	4	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)N2C[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	25022598	95030	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL255007	95030	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at MC4 receptor by cAMP assayAgonist activity at MC4 receptor by cAMP assay	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL500743	214124	0	None	-22	4	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	44456958	97404	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	308	4	1	2	2.8	CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21	10.1021/jm701303z
	CHEMBL269837	97404	0	None	-10	3	Mouse	4.5	pEC50	=	4.5	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	ChEMBL	308	4	1	2	2.8	CCCN1C(=O)C(Cc2ccccc2)NC(=O)c2ccccc21	10.1021/jm701303z
	49862744	15145	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209795	15145	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	11613741	199282	0	None	-223	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.7	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL590281	199282	0	None	-223	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.7	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	16172929	213001	15	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL412536	213001	15	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	11181804	128507	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL366706	128507	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	145988152	167044	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4288909	167044	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	44413828	139293	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL379168	139293	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	90661465	77162	0	None	46	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
	CHEMBL2028958	77162	0	None	46	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
	CHEMBL2078649	77162	0	None	46	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
	44393809	66178	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL184325	66178	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL438920	213809	0	None	-12	4	Human	7.4	pEC50	=	7.4	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
	168295644	192312	0	None	1	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5206336	192312	0	None	1	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	11375529	120151	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL351400	120151	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL427629	213357	0	None	-2	3	Human	6.4	pEC50	=	6.4	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	44405365	71946	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL197278	71946	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	46203213	7958	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1	10.1021/jm9017866
	CHEMBL1090486	7958	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1	10.1021/jm9017866
	CHEMBL1204058	7958	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccnc1	10.1021/jm9017866
	137659790	159322	0	None	-1	4	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4099889	159322	0	None	-1	4	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL5077811	214516	0	None	-87	4	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c00095
	46885863	8472	0	None	41	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1093858	8472	0	None	41	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	25128751	173584	0	None	23	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
	CHEMBL453300	173584	0	None	23	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
	25128748	189991	0	None	8	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
	CHEMBL517108	189991	0	None	8	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
	44577510	188735	0	None	-15	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
	CHEMBL504986	188735	0	None	-15	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
	44275191	81889	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Br)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL216474	81889	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3cc(Br)ccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11330869	119980	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL349886	119980	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44349470	16933	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125308	16933	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44405426	135786	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL373037	135786	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	46884748	8396	0	None	16	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093307	8396	0	None	16	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL3350327	211470	0	None	1	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	45487410	197438	0	None	-12	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	655	16	8	6	1.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569696	197438	0	None	-12	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	655	16	8	6	1.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(C(F)(F)F)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44448477	95557	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257615	95557	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	162643435	181667	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776340	181667	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162643435	181667	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776340	181667	0	None	-4	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	46885416	8280	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	6	1	4	3.6	COCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1092572	8280	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	472	6	1	4	3.6	COCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	90643830	111754	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287337	111754	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	787	10	4	6	2.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL2304250	209486	0	None	-6	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	44409337	170461	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	CHEMBL444883	170461	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
	44349019	114437	0	None	-1	2	Mouse	7.4	pEC50	=	7.4	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL333283	114437	0	None	-1	2	Mouse	7.4	pEC50	=	7.4	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cnnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44394581	122149	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	19	9	6	1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL359702	122149	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	755	19	9	6	1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44322987	96732	0	None	-8	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL264306	96732	0	None	-8	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44322788	157383	0	None	-5	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL407825	157383	0	None	-5	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	90643841	111763	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287348	111763	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	828	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	155563055	175295	0	None	-75	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4573041	175295	0	None	-75	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	9960253	116949	0	None	25	2	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL338594	116949	0	None	25	2	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44349133	117284	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	3.8	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL339545	117284	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	665	11	2	6	3.8	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	137634090	156299	0	None	-2	6	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3980	69	56	64	-22.2	CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2	10.1021/acs.jmedchem.8b00251
	CHEMBL4065418	156299	0	None	-2	6	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assayAgonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	3980	69	56	64	-22.2	CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc4ccccc4)C(=O)NC(=O)[C@H](CSSC[C@@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N3)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N2	10.1021/acs.jmedchem.8b00251
	155512534	169692	0	None	-42	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	642	16	7	6	1.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4437801	169692	0	None	-42	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	642	16	7	6	1.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	46232221	199169	0	None	-1	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL589516	199169	0	None	-1	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	835	12	9	8	-0.1	N=C(N)NCCC[C@@H]1NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	45487290	196780	0	None	-12	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	579	17	9	7	-1.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL565474	196780	0	None	-12	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	579	17	9	7	-1.2	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1c[nH]cn1)C(N)=O	10.1016/j.bmcl.2009.07.025
	11846844	140079	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL380051	140079	0	None	1	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	44405823	72967	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	907	21	8	7	4.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL200668	72967	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	907	21	8	7	4.9	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	11421919	119981	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL349887	119981	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44394654	123973	0	None	9	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	775	20	8	7	1.7	CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL362879	123973	0	None	9	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	775	20	8	7	1.7	CSCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44442978	153076	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397607	153076	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44444448	94063	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	CHEMBL248964	94063	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
	CHEMBL105113	208466	0	None	-1	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	15953833	78974	0	None	8	4	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113037	78974	0	None	8	4	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	46865980	8468	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)C2CN(C(C)(C)C)CC2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1093846	8468	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)C2CN(C(C)(C)C)CC2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	25131477	178701	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
	CHEMBL468252	178701	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
	CHEMBL5075506	214379	0	None	-676	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	168296647	192475	0	None	-213	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5208830	192475	0	None	-213	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	49792705	67503	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	4	1	4	5.5	CC(=O)Nc1cc(-c2ccc(N(C)C)cc2)cn2c(-c3ccc(F)c(Cl)c3)cnc12	nan
	CHEMBL1894685	67503	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	4	1	4	5.5	CC(=O)Nc1cc(-c2ccc(N(C)C)cc2)cn2c(-c3ccc(F)c(Cl)c3)cnc12	nan
	90643803	111743	0	None	-3	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287323	111743	0	None	-3	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	898	18	9	7	0.4	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	46885558	7809	0	None	151	2	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089483	7809	0	None	151	2	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	46885483	8331	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	510	4	1	5	4.1	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1092861	8331	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	510	4	1	5	4.1	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	CHEMBL1204053	8331	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	510	4	1	5	4.1	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
	15603023	97964	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL272660	97964	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	15602927	157882	0	None	1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL408398	157882	0	None	1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	16132144	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	16133793	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	44273719	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.5b01894
	44275263	161926	0	None	478	2	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL415341	161926	0	None	478	2	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	1338	3807	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	9938402	3807	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	CHEMBL339053	3807	43	None	-2	8	Human	8.4	pEC50	=	8.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	44390411	63896	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	CHEMBL180487	63896	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
	44404523	135378	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	882	22	9	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL372785	135378	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	882	22	9	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2005.08.012
	10408	720	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	5329	720	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	9941379	720	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	CHEMBL2070241	720	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	DB11653	720	28	None	-1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
	90643804	111744	0	None	-8	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-8	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	52944242	18153	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269572	18153	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
	56683297	63685	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	CHEMBL1801125	63685	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
	90643808	111747	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643827	111751	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287334	111751	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL5092761	215388	0	None	-295	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	56676631	63669	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1801093	63669	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	56659468	63692	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801145	63692	0	None	-	1	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
	44413931	78015	0	None	9	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL209789	78015	0	None	9	3	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	90643806	111746	0	None	-12	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643805	111745	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	111745	0	None	-1	5	Mouse	8.4	pEC50	=	8.4	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL307457	210981	0	None	-10	4	Mouse	8.4	pEC50	=	8.4	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	CHEMBL5080489	214689	0	None	1	4	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643808	111747	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643805	111745	0	None	1	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287325	111745	0	None	1	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	917	20	11	7	-0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643802	111742	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287322	111742	0	None	-14	5	Human	8.4	pEC50	=	8.4	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	820	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44448590	95599	0	None	25	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL257759	95599	0	None	25	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	11753695	8393	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	CHEMBL1093304	8393	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
	24180493	155124	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL402043	155124	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44394623	141538	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	936	26	11	8	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL384720	141538	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	936	26	11	8	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44322896	167972	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL431801	167972	0	None	1	2	Human	8.3	pEC50	=	8.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	155551699	175140	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4569886	175140	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1680	54	21	19	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	57817763	76927	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70690940	76927	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929808	76927	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070251	76927	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	11296600	122943	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.03.053
	CHEMBL360716	122943	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor Agonistic effective concentration to stimulate cAMP in CHO cells stably expressing the human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.03.053
	11296600	122943	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptorEffective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360716	122943	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptorEffective concentration for cAMP release in HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	11753695	8393	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093304	8393	7	None	-3	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	44441647	154690	0	None	18	3	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL399714	154690	0	None	18	3	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	46203517	7873	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1089891	7873	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204070	7873	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	90643840	111762	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287347	111762	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287061	211300	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287063	211302	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44275263	161926	0	None	478	2	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL415341	161926	0	None	478	2	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11238126	165348	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL423619	165348	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44393850	66097	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL183890	66097	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	10119206	118776	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL341982	118776	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.06.059
	15953833	78974	0	None	8	4	Human	7.4	pEC50	=	7.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113037	78974	0	None	8	4	Human	7.4	pEC50	=	7.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	10119206	118776	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL341982	118776	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL264190	210608	1	None	-30	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	162665450	182296	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784053	182296	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433480	89090	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL236527	89090	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	155568641	176097	0	None	-660	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4591394	176097	0	None	-660	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	162661397	181526	0	None	-70	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4765156	181526	0	None	-70	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	71457994	78579	0	None	1	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	441	8	5	3	3.7	NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1	10.1016/s0960-894x(03)00318-4
	CHEMBL2112213	78579	0	None	1	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cellsAgonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	ChEMBL	441	8	5	3	3.7	NCc1ccc(NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)NCc2ccccc2)cc1	10.1016/s0960-894x(03)00318-4
	11353851	57472	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL165746	57472	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44358630	28314	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL137452	28314	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL541866	28314	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	9958649	124357	0	None	-50	2	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
	CHEMBL363730	124357	0	None	-50	2	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
	71456246	78978	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113040	78978	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	71461652	78980	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113042	78980	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	45487409	196897	0	None	-6	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL566162	196897	0	None	-6	4	Mouse	5.4	pEC50	=	5.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1cccc(Cl)c1)C(N)=O	10.1016/j.bmcl.2009.07.025
	44358630	28314	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL137452	28314	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL541866	28314	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	44358697	12962	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL1189383	12962	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL538589	12962	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL317228	211200	0	None	-10	4	Mouse	4.4	pEC50	=	4.4	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)c1ccccc1	10.1021/jm010524p
	145990599	166855	0	None	-15	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4285535	166855	0	None	-15	4	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	168277543	190675	0	None	-102	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5181752	190675	0	None	-102	4	Human	6.4	pEC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL524861	215623	0	None	-3	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
	162665450	182296	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784053	182296	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44275192	168882	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL438286	168882	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1066	13	11	9	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Br)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	1338	3807	43	None	-2	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	44401323	11800	0	None	72	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1181891	11800	0	None	72	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028961	11800	0	None	72	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44323015	111433	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL327450	111433	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44455892	97919	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL272515	97919	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
	155550083	173914	0	None	-134	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4540411	173914	0	None	-134	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	44397355	127151	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365675	127151	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	11851038	140335	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL184644	209050	0	None	1	3	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CS(=O)(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	56669817	63682	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
	CHEMBL1801122	63682	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
	CHEMBL361252	211834	0	None	4	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CN(C)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44401315	12281	0	None	48	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184825	12281	0	None	48	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028957	12281	0	None	48	2	Human	7.4	pEC50	=	7.4	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44322994	106997	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL315258	106997	0	None	-4	3	Human	7.4	pEC50	=	7.4	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL2323798	209524	0	None	-13	4	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCN)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	137658252	159629	0	None	-6	3	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	868	10	10	9	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4103508	159629	0	None	-6	3	Mouse	6.4	pEC50	=	6.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	868	10	10	9	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.6b01707
	44405368	71962	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL197328	71962	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	44443022	154799	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL400249	154799	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	90643823	111721	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287074	111721	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	696	18	9	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NC(Cc1cccc2ccccc12)C(N)=O	10.1021/jm500064t
	45487292	196852	0	None	-20	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	628	16	9	8	-0.3	N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL565900	196852	0	None	-20	3	Mouse	4.4	pEC50	=	4.4	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	628	16	9	8	-0.3	N#C/C(=C\c1ccc(O)cc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](CCCNC(=N)N)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL455070	213999	0	None	25	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	CHEMBL3287069	211307	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)c(I)c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	137656521	159744	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4104927	159744	0	None	12	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1139	22	17	16	-3.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44397660	123431	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL361731	123431	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	11692334	200428	0	None	-275	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	5	1	4	4.6	O=C1C(Cc2n[nH]c3cc(F)ccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL598214	200428	0	None	-275	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	5	1	4	4.6	O=C1C(Cc2n[nH]c3cc(F)ccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL488355	214075	0	None	-43	3	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C(C)(C)C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44456336	156098	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	CHEMBL406309	156098	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
	49862478	15075	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	CHEMBL1209458	15075	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
	44409240	74434	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	CHEMBL202699	74434	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	44444502	154916	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL400933	154916	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44409240	74434	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
	CHEMBL202699	74434	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
	59077913	89470	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	845	21	8	7	2.7	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL2371886	89470	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	845	21	8	7	2.7	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44409240	74434	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
	CHEMBL202699	74434	0	None	457	3	Human	7.4	pEC50	=	7.4	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
	11249788	120114	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL351088	120114	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	11753668	120369	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL353239	120369	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	11364802	165289	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL423250	165289	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL2370967	209970	0	None	-3	2	Human	7.4	pEC50	=	7.4	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	11599302	199369	0	None	66	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.4	COC1(Cc2n[nH]c3ccccc23)C(=O)N(CC(=O)N(c2ccc(F)cc2)C(C)C)C=CN(c2ccccc2)C1=O	10.1016/j.bmc.2010.01.049
	CHEMBL590841	199369	0	None	66	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	555	8	1	5	4.4	COC1(Cc2n[nH]c3ccccc23)C(=O)N(CC(=O)N(c2ccc(F)cc2)C(C)C)C=CN(c2ccccc2)C1=O	10.1016/j.bmc.2010.01.049
	CHEMBL5078687	214580	0	None	-4	4	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	90643827	111751	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287334	111751	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	920	15	7	6	1.9	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44349106	116878	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	623	9	3	6	3.6	CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL338274	116878	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	623	9	3	6	3.6	CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	44405362	168283	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL433991	168283	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	44349105	17127	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	649	8	3	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)C(F)(F)F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL125529	17127	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	649	8	3	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)C(F)(F)F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL3287067	211305	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL184326	209049	0	None	3	3	Human	6.4	pEC50	=	6.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		COP(=S)(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)OC	10.1016/j.bmcl.2004.07.046
	71459896	78539	0	None	6	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL2112064	78539	0	None	6	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/s0960-894x(02)00830-2
	44415991	80510	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL214770	80510	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
	44415991	80510	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
	CHEMBL214770	80510	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
	44275371	141904	0	None	10	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1032	14	11	10	0.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3N(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL386871	141904	0	None	10	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1032	14	11	10	0.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3N(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885760	8278	0	None	102	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
	CHEMBL1092550	8278	0	None	102	2	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
	44394783	126373	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	847	23	9	6	4.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365044	126373	0	None	-1	3	Human	7.4	pEC50	=	7.4	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	847	23	9	6	4.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44372964	51747	0	None	20	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL158471	51747	0	None	20	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	73354716	89475	0	None	18	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	CHEMBL2372039	89475	0	None	18	2	Human	7.4	pEC50	=	7.4	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	820	21	9	7	1.3	CCCCC(=O)N[C@@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.012
	CHEMBL5094168	215479	0	None	-134	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44433388	88572	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
	CHEMBL235432	88572	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
	44444511	94009	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL248687	94009	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44310242	156309	0	None	-16	3	Mouse	6.4	pEC50	=	6.4	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932912	156309	0	None	-16	3	Mouse	6.4	pEC50	=	6.4	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL406550	156309	0	None	-16	3	Mouse	6.4	pEC50	=	6.4	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL364359	211922	0	None	-2	3	Human	5.3	pEC50	=	5.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NS(=O)(=O)C(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44413831	78064	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL210008	78064	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
	46885815	7860	0	None	25	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	CHEMBL1089830	7860	0	None	25	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	CHEMBL3287065	211304	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	44405360	133561	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	CHEMBL371063	133561	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
	137659790	159322	0	None	-1	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL4099889	159322	0	None	-1	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44394080	126766	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL365279	126766	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL3349030	211405	0	None	-1	3	Human	6.3	pEC50	=	6.3	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	11477853	66894	0	None	-7	2	Human	5.3	pEC50	=	5.3	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
	CHEMBL186439	66894	0	None	-7	2	Human	5.3	pEC50	=	5.3	Functional	Agonistic activity for human Melanocortin 4 receptor as stimulated cAMP releaseAgonistic activity for human Melanocortin 4 receptor as stimulated cAMP release	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
	46885323	8209	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092209	8209	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	51346770	58227	0	None	-29	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
	CHEMBL1682209	58227	0	None	-29	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
	137659790	159322	0	None	-1	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4099889	159322	0	None	-1	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	137646333	157922	0	None	-13	2	Human	4.3	pEC50	=	4.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4084386	157922	0	None	-13	2	Human	4.3	pEC50	=	4.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	49862425	15060	0	None	74	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209382	15060	0	None	74	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	25133207	172943	0	None	15	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
	CHEMBL451694	172943	0	None	15	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
	168277258	190710	0	None	-10	4	Human	7.3	pEC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5182345	190710	0	None	-10	4	Human	7.3	pEC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	90643808	111747	0	None	-14	5	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44349057	16815	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	617	8	2	7	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc(Cl)c2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL124688	16815	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	617	8	2	7	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc(Cl)c2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44397338	123677	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL362129	123677	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	45487297	197101	0	None	-9	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	613	17	8	6	0.7	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL567634	197101	0	None	-9	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	613	17	8	6	0.7	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	137659394	159534	0	None	-12	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4102353	159534	0	None	-12	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	52947911	18152	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	CHEMBL1269571	18152	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptorAgonist activity at human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
	CHEMBL491870	214077	0	None	-9	5	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287067	211305	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44275312	141407	0	None	70	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL384036	141407	0	None	70	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	11456260	156496	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL406764	156496	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44442941	152725	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397312	152725	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	71459938	78981	0	None	4	4	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113043	78981	0	None	4	4	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL311629	211100	0	None	-56	2	Human	5.3	pEC50	=	5.3	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	3794549	34115	6	None	-	1	Human	4.3	pEC50	=	4.3	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	337	3	2	5	3.7	CCc1ccc(C2CC(c3ccc(F)cc3)Nc3nc(N)nn32)cc1	nan
	CHEMBL1425554	34115	6	None	-	1	Human	4.3	pEC50	=	4.3	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	337	3	2	5	3.7	CCc1ccc(C2CC(c3ccc(F)cc3)Nc3nc(N)nn32)cc1	nan
	CHEMBL3601431	211827	0	None	-1	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	44394081	66226	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL184526	66226	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL5081077	214717	0	None	-89	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	1338	3807	43	None	-2	8	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	9938402	3807	43	None	-2	8	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	CHEMBL339053	3807	43	None	-2	8	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 D122A mutant expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
	46232226	201083	0	None	-6	4	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL602853	201083	0	None	-6	4	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	863	12	9	8	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	71454492	78955	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113008	78955	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
	11179914	120182	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	CHEMBL351705	120182	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
	44397702	124085	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL363280	124085	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL3287068	211306	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	90643815	111719	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287066	111719	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	707	15	8	6	1.1	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL3287062	211301	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	122184633	122432	0	None	-4	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600914	122432	0	None	-4	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
	25132864	172602	0	None	42	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
	CHEMBL449050	172602	0	None	42	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
	25132866	172611	0	None	20	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
	CHEMBL449131	172611	0	None	20	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
	CHEMBL2371880	210144	0	None	147	2	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(cccc3OC)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885481	7755	0	None	12	2	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089104	7755	0	None	12	2	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44457067	97742	0	None	5	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	CHEMBL271586	97742	0	None	5	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cellsAgonist activity at mouse MC4R expressed in HEK293 cells	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
	44405770	135448	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	22	9	7	2.9	NC(=O)CCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL372829	135448	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	896	22	9	7	2.9	NC(=O)CCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@]1(NC(=O)Cc2ccccc2)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44405812	135752	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL373016	135752	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	848	22	9	7	2.5	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44394624	97016	0	None	-100	3	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	964	27	11	9	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL266665	97016	0	None	-100	3	Human	8.3	pEC50	=	8.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	964	27	11	9	2.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44401520	13930	0	None	181	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1196472	13930	0	None	181	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL557154	13930	0	None	181	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	44401524	14006	0	None	120	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1197052	14006	0	None	120	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL559181	14006	0	None	120	2	Human	8.3	pEC50	=	8.3	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44404525	168656	0	None	257	2	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	864	22	10	8	2.2	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(O)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL436329	168656	0	None	257	2	Human	8.3	pEC50	=	8.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	864	22	10	8	2.2	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(O)cc2)CC1	10.1016/j.bmcl.2005.08.012
	168281389	190922	0	None	-17	4	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5185405	190922	0	None	-17	4	Human	8.3	pEC50	=	8.3	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
	1324	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	90643824	111748	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287330	111748	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	842	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44456102	155604	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL404549	155604	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	90643808	111747	0	None	-14	5	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-14	5	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643806	111746	0	None	-8	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-8	5	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44349173	116990	0	None	3	3	Human	8.3	pEC50	=	8.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
	CHEMBL338768	116990	0	None	3	3	Human	8.3	pEC50	=	8.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
	CHEMBL410672	212830	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)Agonist activity at human Melanocortin-4 receptor as peptide required for 50% maximal cAMP release (n > or =2)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
	44408173	75401	0	None	154	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL203975	75401	0	None	154	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	145966490	164362	0	None	1	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4212762	164362	0	None	1	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL3287072	211308	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	16132144	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	16133793	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	44273719	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm010524p
	16132144	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	16133793	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	44273719	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303608
	49862375	15039	0	None	16	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209318	15039	0	None	16	4	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	16132144	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	16133793	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	44273719	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2003.08.078
	127047209	139812	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798845	139812	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL264190	210608	1	None	-2	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.0c02041
	44408155	140553	0	None	114	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
	CHEMBL381125	140553	0	None	114	4	Human	8.3	pEC50	=	8.3	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
	1323	2688	55	None	-36	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
	92432	2688	55	None	-36	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
	CHEMBL430239	2688	55	None	-36	8	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
	CHEMBL264190	210608	1	None	-2	8	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	CHEMBL503449	214166	0	None	-1	4	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	137633806	156481	0	None	10	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	CHEMBL4067491	156481	0	None	10	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1031	14	14	13	-2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00353
	44413876	79744	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	CHEMBL211699	79744	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
	44413876	79744	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
	CHEMBL211699	79744	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
	127046235	139638	0	None	-10	5	Mouse	8.2	pEC50	=	8.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3797690	139638	0	None	-10	5	Mouse	8.2	pEC50	=	8.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	1338	3807	43	None	-2	8	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
	9938402	3807	43	None	-2	8	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
	CHEMBL339053	3807	43	None	-2	8	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
	44408190	96923	0	None	46	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL265985	96923	0	None	46	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	44408154	141362	0	None	218	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
	CHEMBL383719	141362	0	None	218	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
	155532197	171739	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1998	72	23	25	-0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4467240	171739	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAgonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1998	72	23	25	-0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	44442965	149659	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
	CHEMBL394744	149659	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
	10257242	15030	0	None	39	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209252	15030	0	None	39	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL2370968	209971	0	None	-6	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assayAgonist activity at human MC4R transfected in HEK293 cells assessed as cAMP accumulation by competitive binding assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	CHEMBL2323786	209512	0	None	-3	4	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	44405785	72706	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL199740	72706	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44394785	124040	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	865	22	9	7	3.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL363061	124040	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	865	22	9	7	3.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL2370968	209971	0	None	-6	4	Human	7.3	pEC50	=	7.3	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	168278924	191066	0	None	-33	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5187368	191066	0	None	-33	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	155531140	171618	0	None	-1	4	Mouse	6.3	pEC50	=	6.3	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	666	16	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	CHEMBL4465466	171618	0	None	-1	4	Mouse	6.3	pEC50	=	6.3	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	666	16	8	7	0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	44358609	28779	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL137855	28779	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	155549865	173856	0	None	-125	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	658	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4539175	173856	0	None	-125	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	658	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155561743	175772	0	None	-389	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4583714	175772	0	None	-389	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL106959	208474	0	None	-3	3	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)C(c1ccccc1)c1ccccc1	10.1021/jm010524p
	1337	3424	6	None	-14	5	Rat	5.3	pEC50	=	5.3	Functional	Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	3424	6	None	-14	5	Rat	5.3	pEC50	=	5.3	Functional	Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	3424	6	None	-14	5	Rat	5.3	pEC50	=	5.3	Functional	Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	11845440	138672	0	None	-4	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
	CHEMBL377778	138672	0	None	-4	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
	137640703	157097	0	None	-338	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4074479	157097	0	None	-338	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487294	196813	0	None	-5	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	601	17	8	6	0.5	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL565688	196813	0	None	-5	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	601	17	8	6	0.5	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	46203515	8041	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1090886	8041	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204068	8041	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3F)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44393851	123089	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360989	123089	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL406891	212626	0	None	-23	5	Mouse	7.3	pEC50	=	7.3	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(N)=O	10.1021/jm030452x
	44413832	78065	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL210009	78065	0	None	2	3	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	44444505	94508	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL251594	94508	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL322610	211234	0	None	-2	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	46885974	8121	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091633	8121	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	474	4	1	3	4.5	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	10210972	12275	0	None	19	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL1184771	12275	0	None	19	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145454	12275	0	None	19	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
	44391929	12412	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1185810	12412	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL2145453	12412	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44396987	67193	0	None	22	3	Human	7.3	pEC50	=	7.3	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL187774	67193	0	None	22	3	Human	7.3	pEC50	=	7.3	Functional	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
	CHEMBL5094215	215481	0	None	-15	4	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44348845	116880	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL338277	116880	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	45487414	197281	0	None	-4	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL568577	197281	0	None	-4	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	621	16	8	6	0.8	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccc(Cl)cc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	137636965	156216	0	None	-5	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4064433	156216	0	None	-5	4	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487405	197437	0	None	-43	3	Mouse	4.3	pEC50	=	4.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	587	16	8	6	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	CHEMBL569695	197437	0	None	-43	3	Mouse	4.3	pEC50	=	4.3	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	587	16	8	6	0.1	N=C(N)NCCC[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)/C=C/c1ccccc1)C(N)=O	10.1016/j.bmcl.2009.07.025
	56659465	63670	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801094	63670	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
	46202891	7707	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	500	4	1	4	4.8	COc1ccc([C@]2(O)[C@@H](C)CN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)C[C@H]2C)cc1	10.1021/jm9017866
	CHEMBL1088830	7707	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	500	4	1	4	4.8	COc1ccc([C@]2(O)[C@@H](C)CN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)C[C@H]2C)cc1	10.1021/jm9017866
	CHEMBL1204060	7707	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	500	4	1	4	4.8	COc1ccc([C@]2(O)[C@@H](C)CN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)C[C@H]2C)cc1	10.1021/jm9017866
	11851038	140335	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44275488	159127	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL409786	159127	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	44322924	107112	0	None	-7	3	Human	7.3	pEC50	=	7.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL316038	107112	0	None	-7	3	Human	7.3	pEC50	=	7.3	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL2370965	209968	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
	CHEMBL204263	209163	0	None	-87	4	Human	6.3	pEC50	=	6.3	Functional	Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulationActivity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
	44349461	16896	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125079	16896	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	44405361	135037	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	CHEMBL371945	135037	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
	11635051	200396	0	None	-2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	CHEMBL598021	200396	0	None	-2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	525	7	1	4	4.6	CC(C)N(C(=O)CN1C=CN(c2ccccc2)C(=O)C(Cc2n[nH]c3cc(F)ccc23)C1=O)c1ccccc1	10.1016/j.bmc.2010.01.049
	44413829	78066	0	None	-1	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL210011	78066	0	None	-1	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
	CHEMBL3287060	211299	0	None	1	5	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL2323791	209517	0	None	-4	4	Mouse	5.3	pEC50	=	5.3	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	44441685	94132	0	None	-1	3	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL249322	94132	0	None	-1	3	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL264190	210608	1	None	-30	8	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	46885367	7852	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1089797	7852	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44397653	66992	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL186876	66992	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397412	67311	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL188395	67311	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44404529	72427	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	749	18	8	6	2.0	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198776	72427	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	749	18	8	6	2.0	NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	73347133	89472	0	None	-7	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371903	89472	0	None	-7	2	Human	7.3	pEC50	=	7.3	Functional	Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulationAgonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation	ChEMBL	960	13	10	9	0.9	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2c3ccccc3CN2C1=O	10.1016/s0960-894x(03)00114-8
	44441683	94130	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL249320	94130	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
	44449216	95271	0	None	2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL256286	95271	0	None	2	2	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	90643836	111758	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287343	111758	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL2369485	209628	0	None	-3	4	Mouse	7.2	pEC50	=	7.2	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	44441687	94005	0	None	43	2	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL248671	94005	0	None	43	2	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	44442934	93768	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL247422	93768	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	10098568	15018	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209194	15018	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	90643829	111753	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287336	111753	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL2112008	209226	0	None	-1	3	Human	6.2	pEC50	=	6.2	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	44405526	72409	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL198723	72409	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL194552	209099	0	None	-1	2	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP levelAgonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
	44393862	123681	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL362147	123681	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	54584302	60812	0	None	28	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
	CHEMBL1761874	60812	0	None	28	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
	44394784	126295	0	None	-2	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	861	23	9	7	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365019	126295	0	None	-2	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	861	23	9	7	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL5093939	215458	0	None	-77	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	CHEMBL5075712	214394	0	None	-102	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44443014	154010	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL398409	154010	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	11296732	143813	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	CHEMBL390130	143813	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	164624627	185879	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4868223	185879	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	44358848	118984	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL342470	118984	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL50056	214119	2	None	-4	7	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm060384p
	24848995	117947	0	None	1	2	Mouse	7.2	pEC50	=	7.2	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL340355	117947	0	None	1	2	Mouse	7.2	pEC50	=	7.2	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL183733	209047	0	None	-4	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL50056	214119	2	None	-4	7	Human	7.2	pEC50	=	7.2	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	44442942	93599	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL246605	93599	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	44405377	72024	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	CHEMBL197541	72024	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
	44456183	98022	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL272956	98022	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	44275488	159127	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL409786	159127	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1039	16	11	9	2.2	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885759	8276	0	None	95	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	CHEMBL1092548	8276	0	None	95	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
	46885482	8330	0	None	81	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092860	8330	0	None	81	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44404524	136076	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	907	24	9	8	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC(C)C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL373212	136076	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	907	24	9	8	3.3	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC(C)C)cc2)CC1	10.1016/j.bmcl.2005.08.012
	6918813	131371	3	None	77	4	Human	8.2	pEC50	=	8.2	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL368876	131371	3	None	77	4	Human	8.2	pEC50	=	8.2	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL217584	209377	0	None	-2	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptorEffective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
	44408276	75507	0	None	61	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	CHEMBL204308	75507	0	None	61	4	Human	8.2	pEC50	=	8.2	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
	90643804	111744	0	None	-8	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287324	111744	0	None	-8	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287327	211310	0	None	-5	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	71449047	78480	0	None	28	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
	CHEMBL2111807	78480	0	None	28	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
	16132144	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	16133793	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	44273719	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	CHEMBL214332	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	137638725	156979	0	None	3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4073016	156979	0	None	3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL3287060	211299	0	None	1	5	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44348200	160196	0	None	-2	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
	CHEMBL410949	160196	0	None	-2	3	Human	8.2	pEC50	=	8.2	Functional	Effective concentration of peptide at 50% maximal cAMP generationEffective concentration of peptide at 50% maximal cAMP generation	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
	44322787	105964	0	None	1	3	Human	8.2	pEC50	=	8.2	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL312998	105964	0	None	1	3	Human	8.2	pEC50	=	8.2	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	137647009	157854	0	None	30	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4083755	157854	0	None	30	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	1324	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16154396	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	16197727	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	44285019	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	57514683	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	91898441	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL441738	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	DB04931	302	25	None	-14	9	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	49862377	15041	0	None	13	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209320	15041	0	None	13	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
	44441681	94129	0	None	104	2	Human	8.2	pEC50	=	8.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL249319	94129	0	None	104	2	Human	8.2	pEC50	=	8.2	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	44444510	155132	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL402060	155132	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	11851038	140335	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL3287342	211313	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	145975465	163949	0	None	6	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4207725	163949	0	None	6	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	145964837	164347	0	None	1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4212629	164347	0	None	1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL5080784	214706	0	None	-2	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	44444500	94144	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL249370	94144	0	None	-	1	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	54584301	60810	0	None	24	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
	CHEMBL1761872	60810	0	None	24	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
	10101361	155703	0	None	1	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL405174	155703	0	None	1	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44373197	119473	0	None	-16	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL345234	119473	0	None	-16	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	44390423	63764	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL180157	63764	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL5085972	215003	0	None	-1	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.1c00095
	168290510	191897	0	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	CHEMBL5199932	191897	0	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
	44277301	100856	0	None	3	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29349	100856	0	None	3	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	854	21	9	7	2.0	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Cl)cccc2C1	10.1016/s0960-894x(02)00830-2
	44349094	17937	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	589	9	3	6	3.0	COCC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL125935	17937	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	589	9	3	6	3.0	COCC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	155547842	173696	0	None	-251	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	741	17	10	7	-1.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4535510	173696	0	None	-251	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	741	17	10	7	-1.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1CCC[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155556047	174497	0	None	-199	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4554828	174497	0	None	-199	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162669064	182737	0	None	-	1	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	684	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	CHEMBL4789938	182737	0	None	-	1	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL	684	16	8	7	-0.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O	10.1021/acsmedchemlett.0c00561
	1337	3424	6	None	-15	5	Mouse	5.2	pEC50	=	5.2	Functional	Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	6918851	3424	6	None	-15	5	Mouse	5.2	pEC50	=	5.2	Functional	Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	CHEMBL364346	3424	6	None	-15	5	Mouse	5.2	pEC50	=	5.2	Functional	Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R)	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
	137636677	156100	0	None	-75	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4063111	156100	0	None	-75	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	45487408	196854	0	None	-16	3	Mouse	4.2	pEC50	=	4.2	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	CHEMBL565927	196854	0	None	-16	3	Mouse	4.2	pEC50	=	4.2	Functional	Agonistic activity against mouse MC4RAgonistic activity against mouse MC4R	ChEMBL	617	17	8	7	0.1	COc1ccc(/C=C\C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(N)=O)cc1	10.1016/j.bmcl.2009.07.025
	46885907	8040	0	None	104	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1090885	8040	0	None	104	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44397410	124359	0	None	31	3	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL363740	124359	0	None	31	3	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	168285801	191481	0	None	-12	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
	CHEMBL5193501	191481	0	None	-12	4	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
	57817773	76925	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70684623	76925	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929806	76925	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070249	76925	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885761	8028	0	None	56	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
	CHEMBL1090813	8028	0	None	56	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
	CHEMBL3287063	211302	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL2448525	210499	0	None	-95	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	46885817	7907	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	3	1	3	4.3	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1090162	7907	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	436	3	1	3	4.3	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	44390422	63468	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL179837	63468	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL5077811	214516	0	None	-87	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c00095
	137648144	157758	0	None	38	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4082585	157758	0	None	38	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL455826	214009	0	None	-1	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cc2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44397459	125794	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL364789	125794	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL413439	213070	0	None	-64	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	2891887	55374	6	None	2	2	Human	5.2	pEC50	=	5.2	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	494	7	1	5	4.7	O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3ccccc3c2)CC1	nan
	CHEMBL1380969	55374	6	None	2	2	Human	5.2	pEC50	=	5.2	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	494	7	1	5	4.7	O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3ccccc3c2)CC1	nan
	CHEMBL1619128	55374	6	None	2	2	Human	5.2	pEC50	=	5.2	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	494	7	1	5	4.7	O=C1c2cccc3cccc(c23)C(=O)N1CC1CCN(CC(O)COc2ccc3ccccc3c2)CC1	nan
	44393820	66678	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185427	66678	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	46232223	199164	0	None	-2	3	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	9	8	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	CHEMBL589468	199164	0	None	-2	3	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL	849	12	9	8	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)CCCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmc.2009.12.010
	90643839	111761	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	7	2	5	3.7	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287346	111761	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	717	7	2	5	3.7	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL138212	208752	0	None	-11	3	Mouse	6.2	pEC50	=	6.2	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(N)=O	10.1016/j.bmcl.2003.08.078
	46203212	8277	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(C#N)c1	10.1021/jm9017866
	CHEMBL1092549	8277	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(C#N)c1	10.1021/jm9017866
	CHEMBL1204063	8277	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	495	3	1	4	4.7	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(C#N)c1	10.1021/jm9017866
	73354704	89474	0	None	13	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	989	13	11	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL2371913	89474	0	None	13	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	989	13	11	9	0.8	CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44275654	157334	0	None	5	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	11	9	0.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL407754	157334	0	None	5	2	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	975	13	11	9	0.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	73350149	89453	0	None	2	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2371220	89453	0	None	2	2	Human	7.2	pEC50	=	7.2	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	10146483	64178	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	CHEMBL180854	64178	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
	1334	1501	7	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16133814	1501	7	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL437050	1501	7	None	-6	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	53318436	58803	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	814	17	10	9	-0.4	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O	10.1021/jm101425m
	CHEMBL1688108	58803	0	None	-3	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	814	17	10	9	-0.4	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSCC(=O)N([C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C[C@H](CCCNC(=N)N)NC1=O	10.1021/jm101425m
	164619151	185554	0	None	-2	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	610	11	4	4	5.5	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4863206	185554	0	None	-2	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	610	11	4	4	5.5	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	44349183	18535	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	632	8	4	7	3.7	CCOC(=O)NC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	CHEMBL127491	18535	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	632	8	4	7	3.7	CCOC(=O)NC(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/s0960-894x(03)00796-0
	155549385	173805	0	None	-117	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4538225	173805	0	None	-117	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL3287342	211313	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	90643826	111750	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287333	111750	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	839	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3600922	211825	0	None	-9	4	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	71456245	78976	0	None	2	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113039	78976	0	None	2	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	46228815	199362	0	None	-52	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	556	8	1	6	4.1	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL590794	199362	0	None	-52	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	556	8	1	6	4.1	COc1ccc(N(C(=O)CN2C=CN(c3cccnc3)C(=O)C(Cc3n[nH]c4cc(F)ccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	44443021	94121	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL249267	94121	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL302703	210914	0	None	-20	5	Mouse	5.2	pEC50	=	5.2	Functional	Functional activity at the mouse melanocortin 4 receptorFunctional activity at the mouse melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010061n
	44444504	154917	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL400934	154917	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	44448515	155444	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL403834	155444	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
	122184910	122555	0	None	-2	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601428	122555	0	None	-2	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	10008561	15016	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209192	15016	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	164628926	186513	0	None	-3	3	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	543	14	3	3	6.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C	10.1021/acs.jmedchem.0c02041
	CHEMBL4877537	186513	0	None	-3	3	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	543	14	3	3	6.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2CC(C)C)C(=N)N1CCCC(C)C	10.1021/acs.jmedchem.0c02041
	137636428	156040	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4062443	156040	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL319871	211224	0	None	-5	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	44394586	126779	0	None	7	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	759	20	8	7	1.0	COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL365385	126779	0	None	7	3	Human	7.2	pEC50	=	7.2	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	759	20	8	7	1.0	COCC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL3287072	211308	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44349056	16806	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	651	8	2	7	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL124633	16806	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	651	8	2	7	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	44397570	122909	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL360603	122909	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	137649543	157320	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4077331	157320	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1025	18	12	15	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	46203516	8088	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091281	8088	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204069	8088	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	478	4	1	3	4.3	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(F)c(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	46885972	8119	0	None	10	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091631	8119	0	None	10	4	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44349107	116879	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	637	10	2	6	3.2	CCN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	CHEMBL338275	116879	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	637	10	2	6	3.2	CCN(Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/s0960-894x(03)00796-0
	90643832	111755	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287339	111755	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	51346771	58226	0	None	-57	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
	CHEMBL1682208	58226	0	None	-57	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in BHK cells assessed as stimulation of agonist-induced cAMP accumulation	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
	44275372	96733	0	None	67	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	14	11	9	2.0	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3C(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL264337	96733	0	None	67	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1031	14	11	9	2.0	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3C(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44275175	168833	0	None	186	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1047	15	11	10	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OC(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL437822	168833	0	None	186	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1047	15	11	10	1.6	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(cccc3OC(C)C)C2)NC1=O	10.1016/s0960-894x(03)00114-8
	46885523	7803	0	None	263	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	CHEMBL1089461	7803	0	None	263	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
	11226756	119974	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL349850	119974	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44401530	12795	0	None	51	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1188092	12795	0	None	51	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL535152	12795	0	None	51	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44401528	13989	0	None	61	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1196956	13989	0	None	61	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL558787	13989	0	None	61	2	Human	8.2	pEC50	=	8.2	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	11226756	119974	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL349850	119974	0	None	251	2	Human	8.2	pEC50	=	8.2	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	16132144	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	168283616	191239	0	None	-13	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5190042	191239	0	None	-13	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	127047853	139993	0	None	-4	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3799955	139993	0	None	-4	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	49862743	15144	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209794	15144	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL3287329	211311	0	None	-1	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	90643829	111753	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287336	111753	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	901	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	44323029	207181	0	None	1	3	Human	8.1	pEC50	=	8.1	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	CHEMBL92481	207181	0	None	1	3	Human	8.1	pEC50	=	8.1	Functional	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
	137648144	157758	0	None	38	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4082585	157758	0	None	38	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	1127	22	14	17	-1.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2csc3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	90643808	111747	0	None	-7	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287328	111747	0	None	-7	5	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	1338	3807	43	None	-5	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	9938402	3807	43	None	-5	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	CHEMBL339053	3807	43	None	-5	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/s0960-894x(03)00796-0
	CHEMBL103817	208459	0	None	2	4	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity of compound towards mouse Melanocortin-4 receptor (mMC4R); partial agonistAgonist activity of compound towards mouse Melanocortin-4 receptor (mMC4R); partial agonist	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm010524p
	122179551	121486	0	None	-1	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	CHEMBL3582445	121486	0	None	-1	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.5b00053
	CHEMBL311750	211101	0	None	-4	2	Human	7.2	pEC50	=	7.2	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC/N=C(/N)NC#N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	CHEMBL411359	212879	0	None	1	4	Human	7.2	pEC50	=	7.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
	44357786	116754	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL337571	116754	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assayStimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
	CHEMBL589515	215800	0	None	2	4	Mouse	7.2	pEC50	=	7.2	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2009.12.010
	CHEMBL2323788	209514	0	None	-13	4	Mouse	6.2	pEC50	=	6.2	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	11613526	200488	0	None	-23	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	CHEMBL598631	200488	0	None	-23	2	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	537	8	1	5	4.5	COc1ccc(N(C(=O)CN2C=CN(c3ccccc3)C(=O)C(Cc3n[nH]c4ccccc34)C2=O)C(C)C)cc1	10.1016/j.bmc.2010.01.049
	11295536	57540	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL166328	57540	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	11757528	15017	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209193	15017	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
	90643840	111762	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287347	111762	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	747	16	7	8	1.2	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	44397654	67188	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL187761	67188	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	44397460	126219	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL365004	126219	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	1334	1501	7	None	-6	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	16133814	1501	7	None	-6	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	CHEMBL437050	1501	7	None	-6	4	Human	6.2	pEC50	=	6.2	Functional	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
	44335147	4592	0	None	-4	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	CHEMBL102688	4592	0	None	-4	4	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	ChEMBL	711	16	9	7	-0.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NC1(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm010524p
	46203215	8470	0	None	27	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1093856	8470	0	None	27	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1204065	8470	0	None	27	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44405769	72918	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	957	20	8	7	4.5	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	CHEMBL200449	72918	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	957	20	8	7	4.5	CCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)Nc2ccccc2C(N)=O)CCc2c(Br)cccc2C1	10.1016/j.bmcl.2005.08.083
	44393887	66674	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL185417	66674	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	16132144	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	16133793	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	44273719	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	CHEMBL214332	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2006.04.050
	145971673	164698	0	None	-12	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	837	11	12	9	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL4217191	164698	0	None	-12	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 minsAgonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins	ChEMBL	837	11	12	9	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
	CHEMBL264190	210608	1	None	-30	8	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I102S mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	137643023	158310	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4089119	158310	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1010	16	13	14	-1.1	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)CCC[C@H](N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	46885369	7957	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	5	1	3	4.6	CC(C)CN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	CHEMBL1090485	7957	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	470	5	1	3	4.6	CC(C)CN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
	1334	1501	7	None	-6	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	16133814	1501	7	None	-6	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	CHEMBL437050	1501	7	None	-6	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		None	10.1021/jm500064t
	49862740	15142	0	None	10	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	CHEMBL1209792	15142	0	None	10	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
	137643385	158131	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4087072	158131	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1069	21	13	16	-1.8	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	44433385	89055	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	CHEMBL236489	89055	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISAAgonist activity at human MC4 receptor expressed in CHO cells assessed as cAMP accumulation by ELISA	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
	44349594	116822	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	699	11	0	6	4.5	CC(C)(C)CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL337940	116822	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	699	11	0	6	4.5	CC(C)(C)CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL4299612	213594	0	None	-6	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.5b01894
	44442944	93600	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL246606	93600	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	71456246	78978	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL2113040	78978	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
	137640703	157097	0	None	-338	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4074479	157097	0	None	-338	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL3287062	211301	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	44397659	67119	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL187450	67119	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration at human melanocortin 4 receptor in cAMP release assayEffective concentration at human melanocortin 4 receptor in cAMP release assay	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
	CHEMBL3287068	211306	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	CHEMBL2323796	209522	0	None	-691	3	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL312357	211109	0	None	1	2	Human	6.1	pEC50	=	6.1	Functional	Agonist potency towards human Melanocortin 4 receptorAgonist potency towards human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCCN[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00459-6
	122179549	121484	0	None	-1	2	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1	10.1021/acsmedchemlett.5b00053
	CHEMBL3582443	121484	0	None	-1	2	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assayAgonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	ChEMBL	699	19	10	7	0.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)Cc1ccccc1	10.1021/acsmedchemlett.5b00053
	44372908	119833	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	784	22	10	8	-0.4	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL348526	119833	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	784	22	10	8	-0.4	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(C)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	11050211	34822	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
	CHEMBL143131	34822	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
	90643846	111768	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287353	111768	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	49862664	15123	0	None	60	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209706	15123	0	None	60	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	44442981	153078	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397608	153078	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	102096778	58806	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	51351277	58806	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53322400	58806	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932360	58806	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688111	58806	0	None	-10	4	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	44456410	97439	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL270015	97439	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	90643843	111766	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287350	111766	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	809	13	5	6	2.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	137636428	156040	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4062443	156040	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL264190	210608	1	None	-30	8	Human	6.1	pEC50	=	6.1	Functional	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptoreffective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
	46228689	200219	0	None	-12	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	CHEMBL596794	200219	0	None	-12	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assayAgonist activity at human MC4R expressed in CHO cells after 4 hrs by luciferase reporter gene assay	ChEMBL	519	5	1	4	4.4	O=C1[C@H](Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)C=CN1CC(=O)N1CCCCc2ccccc21	10.1016/j.bmc.2010.01.049
	25132526	188923	0	None	69	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
	CHEMBL507876	188923	0	None	69	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
	44413830	77950	0	None	-1	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL209622	77950	0	None	-1	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL2371887	210145	0	None	52	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL		None	None	None		CCCCC(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@]2(CCc3c(CC)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	44409103	140123	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
	CHEMBL380120	140123	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist potency at MC4 receptorAgonist potency at MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
	11330992	119934	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL349515	119934	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44401310	12785	0	None	125	2	Human	8.1	pEC50	=	8.1	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL1188043	12785	0	None	125	2	Human	8.1	pEC50	=	8.1	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	CHEMBL534930	12785	0	None	125	2	Human	8.1	pEC50	=	8.1	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
	71458041	78891	0	None	-1	2	Human	8.1	pEC50	=	8.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	776	22	10	9	-0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112919	78891	0	None	-1	2	Human	8.1	pEC50	=	8.1	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uMEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation at 50 uM	ChEMBL	776	22	10	9	-0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	168284733	191624	0	None	-35	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL5195641	191624	0	None	-35	4	Human	8.1	pEC50	=	8.1	Functional	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assayAntagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
	CHEMBL3287329	211311	0	None	1	5	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor I69T mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O	10.1021/jm500064t
	49862741	15143	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
	CHEMBL1209793	15143	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
	1338	3807	43	None	-2	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	9938402	3807	43	None	-2	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL339053	3807	43	None	-2	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
	CHEMBL181161	208980	0	None	10	3	Human	8.1	pEC50	=	8.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CNC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44408275	75419	0	None	47	4	Human	8.1	pEC50	=	8.1	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	CHEMBL204078	75419	0	None	47	4	Human	8.1	pEC50	=	8.1	Functional	Activity against human MC4R by cAMP accumulationActivity against human MC4R by cAMP accumulation	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
	1323	2688	55	None	-36	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	92432	2688	55	None	-36	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	CHEMBL430239	2688	55	None	-36	8	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00353
	71461649	78954	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL2113007	78954	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration determined against melanocortin-4 receptorEffective concentration determined against melanocortin-4 receptor	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
	CHEMBL510687	215587	0	None	3	4	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1cccc(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	44415919	141588	0	None	-4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL385000	141588	0	None	-4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	10864861	115200	4	None	128	2	Human	8.1	pEC50	=	8.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
	CHEMBL334457	115200	4	None	128	2	Human	8.1	pEC50	=	8.1	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
	CHEMBL602651	215818	0	None	1	3	Mouse	8.1	pEC50	=	8.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1016/j.bmc.2009.12.010
	16132144	209279	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	16133793	209279	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	44273719	209279	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	CHEMBL214332	209279	36	None	-8	8	Mouse	8.1	pEC50	=	8.1	Functional	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00796-0
	CHEMBL411378	212881	0	None	-16	5	Mouse	8.1	pEC50	=	8.1	Functional	Effective concentration for maximum agonist response towards mouse melanocortin 4 receptorEffective concentration for maximum agonist response towards mouse melanocortin 4 receptor	ChEMBL		None	None	None		Cc1nc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccccc3)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc3ccccc3)NC2=O)c[nH]1	10.1021/jm030452x
	24848995	117947	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	CHEMBL340355	117947	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)Agonistic activity measured as inhibition of cAMP accumulation in HEK cells expressing human Melanocortin 4 receptor (hMC4R)	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/s0960-894x(03)00796-0
	24848995	117947	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL340355	117947	0	None	-1	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	155548791	173730	0	None	-100	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	664	14	6	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4536340	173730	0	None	-100	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	664	14	6	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	44415956	141956	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
	CHEMBL387246	141956	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
	44415956	141956	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	CHEMBL387246	141956	0	None	24	3	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
	46885414	8212	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	5	1	3	4.4	C[C@H]1CN(C(=O)[C@H]2CN(CC3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	CHEMBL1092219	8212	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	468	5	1	3	4.4	C[C@H]1CN(C(=O)[C@H]2CN(CC3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
	44405375	140352	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
	CHEMBL380769	140352	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	cAMP stimulation in HEK293 cells transfected with human MC4RcAMP stimulation in HEK293 cells transfected with human MC4R	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
	90643806	111746	0	None	-12	5	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287326	111746	0	None	-12	5	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor C271Y mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	728	14	5	8	1.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	46885526	7764	0	None	51	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	CHEMBL1089135	7764	0	None	51	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	CHEMBL1204056	7764	0	None	51	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	44394695	123158	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	833	22	9	6	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL361253	123158	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	833	22	9	6	3.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44392015	12778	0	None	41	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL1187982	12778	0	None	41	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	CHEMBL3216179	12778	0	None	41	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cellsEffective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
	44358566	164883	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	CHEMBL422109	164883	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Effective concentration for cAMP accumulation relative to alpha-MSH at human MC4REffective concentration for cAMP accumulation relative to alpha-MSH at human MC4R	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
	164627532	186608	0	None	-18	3	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	11	3	3	6.1	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4878922	186608	0	None	-18	3	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	601	11	3	3	6.1	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H](C(C)C)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL3287065	211304	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(N)=O	10.1021/jm500064t
	44441637	94049	0	None	4	2	Human	6.1	pEC50	=	6.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	CHEMBL248892	94049	0	None	4	2	Human	6.1	pEC50	=	6.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
	25132525	176725	0	None	3	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
	CHEMBL460142	176725	0	None	3	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
	CHEMBL263878	210598	0	None	-2	3	Human	7.1	pEC50	=	7.1	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	44349593	118389	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL341055	118389	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL2304248	209485	0	None	-4	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	137636677	156100	0	None	-75	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4063111	156100	0	None	-75	4	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL2304246	209483	0	None	-1	3	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
	44441688	94354	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	CHEMBL250719	94354	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Antagonist activity at human MC4R assessed as stimulation of cAMP productionAntagonist activity at human MC4R assessed as stimulation of cAMP production	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
	44442943	154681	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL399667	154681	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at MC4R assessed as stimulation of cAMP releaseAgonist activity at MC4R assessed as stimulation of cAMP release	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	122184911	122556	0	None	-1	4	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3601429	122556	0	None	-1	4	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	46942512	72323	0	None	-	1	Human	4.1	pEC50	=	4.1	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	1	4	5.0	CC(=O)Nc1cc(-c2cccnc2)cn2c(-c3cccc(C(F)(F)F)c3)cnc12	nan
	CHEMBL1984089	72323	0	None	-	1	Human	4.1	pEC50	=	4.1	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	1	4	5.0	CC(=O)Nc1cc(-c2cccnc2)cn2c(-c3cccc(C(F)(F)F)c3)cnc12	nan
	59149266	76926	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	70693081	76926	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	91929807	76926	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	CHEMBL2070250	76926	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	46885906	8475	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	4	1	3	4.0	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1093888	8475	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	4	1	3	4.0	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1204066	8475	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	442	4	1	3	4.0	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	51351151	58805	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	53318437	58805	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	91932359	58805	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	CHEMBL1688110	58805	0	None	-2	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay	ChEMBL	1635	23	20	21	-1.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCNC(=N)N)NC(=O)[C@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm101425m
	44405825	140930	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL382273	140930	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	921	22	8	7	4.6	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCc2ccc(C(N)=O)cc2)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL5092761	215388	0	None	-295	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assayAgonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
	16157270	212553	14	None	-575	7	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/acs.jmedchem.5b01894
	CHEMBL405282	212553	14	None	-575	7	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/acs.jmedchem.5b01894
	137641157	157064	0	None	-24	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4074074	157064	0	None	-24	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF methodAgonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL2070374	209187	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albuminAgonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
	9919056	72073	0	None	14	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL197695	72073	0	None	14	2	Human	7.1	pEC50	=	7.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL183315	209043	0	None	6	3	Human	7.1	pEC50	=	7.1	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	44448554	155372	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	CHEMBL403421	155372	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as cAMP releaseAgonist activity at human MC4R expressed in CHO cells assessed as cAMP release	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
	44359591	32075	0	None	-1	3	Mouse	6.1	pEC50	=	6.1	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	699	19	8	7	-0.2	CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	CHEMBL140847	32075	0	None	-1	3	Mouse	6.1	pEC50	=	6.1	Functional	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cellsAgonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	ChEMBL	699	19	8	7	-0.2	CC(=O)N(CCc1c[nH]cn1)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.08.078
	46885525	7763	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	4	1	5	3.5	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1089134	7763	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	4	1	5	3.5	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	CHEMBL1204055	7763	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	458	4	1	5	3.5	CC(C)[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
	16132144	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	16133793	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	44273719	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	CHEMBL214332	209279	36	None	-12	8	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
	90643832	111755	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287339	111755	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	44349469	17093	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	CHEMBL125492	17093	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Intracellular level of cAMP in cells expressing the melanocortin 4 receptorIntracellular level of cAMP in cells expressing the melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
	137647009	157854	0	None	30	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4083755	157854	0	None	30	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1122	22	14	16	-1.6	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	11156852	65685	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	CHEMBL183434	65685	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as stimulation of cAMP production	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
	44416152	81098	0	None	15	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	CHEMBL215576	81098	0	None	15	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4RAgonist activity at human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
	44444499	155013	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL401466	155013	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	25129108	172696	0	None	4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
	CHEMBL450236	172696	0	None	4	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assayAgonist activity at human MC4R expressed in HEK293 cells assessed as effect on CRE-driven luminescence by luciferase reporter gene assay	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
	11847001	80228	0	None	125	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL213747	80228	0	None	125	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	44275263	161926	0	None	478	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	CHEMBL415341	161926	0	None	478	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human melanocortin receptor (hMC4R).Agonist activity at human melanocortin receptor (hMC4R).	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
	1324	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16154396	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	16197727	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	44285019	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	57514683	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	91898441	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	CHEMBL441738	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	DB04931	302	25	None	-14	9	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		None	10.1021/jm050780s
	10169912	72425	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL198771	72425	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cellsEffective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells	ChEMBL	878	23	9	8	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OC)cc2)CC1	10.1016/j.bmcl.2005.08.012
	CHEMBL410168	212804	0	None	4	3	Human	8.1	pEC50	=	8.1	Functional	Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.Intracellular cAMP accumulation in Melanocortin 4 receptor functional assay.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
	44456184	155488	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL404069	155488	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP productionAgonist activity at human MC4 receptor expressed in CHO cells assessed as accumulation of cAMP production	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	49862375	15039	0	None	16	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	CHEMBL1209318	15039	0	None	16	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
	16132144	209279	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	16133793	209279	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	44273719	209279	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	CHEMBL214332	209279	36	None	-12	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.7b00353
	137635422	155910	0	None	30	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060816	155910	0	None	30	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1111	22	15	16	-2.3	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4299619	213595	0	None	-4	4	Mouse	8.0	pEC50	=	8.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL266288	96963	0	None	-	1	Mouse	8.0	pEC50	=	8.0	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	5507	70	67	87	-15.6	CSCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CSSSSC[C@@H]3NC(=O)[C@@H]4CCCN4C(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](CSSSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(N)=O)NC1=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CSSSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N4)NC3=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSSSC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCN=C(N)N)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/jm0303608
	11851038	140335	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAgonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL438596	213781	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
	137637026	155925	0	None	28	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4060937	155925	0	None	28	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1052	20	15	14	-1.4	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	90643837	111759	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	CHEMBL3287344	111759	0	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	750	11	3	7	3.4	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O	10.1021/jm500064t
	11017471	31917	0	None	295	2	Human	8.0	pEC50	=	8.0	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
	CHEMBL140738	31917	0	None	295	2	Human	8.0	pEC50	=	8.0	Functional	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
	49862378	15042	0	None	45	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL1209321	15042	0	None	45	4	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulationAgonist activity at human MC4 receptor expressed in CHO cells assessed as increase of alpha-MSH-induced cAMP accumulation	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
	CHEMBL264190	210608	1	None	-30	8	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at human melanocortin-4 receptor A219V mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm500064t
	49862738	15140	0	None	36	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209790	15140	0	None	36	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	56673304	63680	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
	CHEMBL1801120	63680	0	None	-	1	Human	8.0	pEC50	=	8	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 minsAgonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
	44277300	101352	0	None	16	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	850	22	9	8	1.3	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC)C1	10.1016/s0960-894x(02)00830-2
	CHEMBL29693	101352	0	None	16	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity against human melanocortin receptor hMC4RAgonist activity against human melanocortin receptor hMC4R	ChEMBL	850	22	9	8	1.3	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2OC)C1	10.1016/s0960-894x(02)00830-2
	155553683	174183	0	None	-295	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4547556	174183	0	None	-295	4	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL3287060	211299	0	None	-1	5	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assayAgonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acsmedchemlett.9b00198
	11851038	140335	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	CHEMBL380691	140335	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAgonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
	44405791	168651	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	CHEMBL436296	168651	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity in HEK293 cells transfected with human MC4R by cAMP accumulationAgonist activity in HEK293 cells transfected with human MC4R by cAMP accumulation	ChEMBL	859	22	8	7	3.1	CCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)NCCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.083
	44393876	122567	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL360169	122567	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	155551195	173942	0	None	-426	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	626	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4541098	173942	0	None	-426	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	626	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155560756	175085	0	None	-177	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4568647	175085	0	None	-177	4	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assayAgonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay	ChEMBL	756	14	6	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	122184635	122434	0	None	-56	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600916	122434	0	None	-56	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	44444509	93968	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	CHEMBL248435	93968	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human MC4R expressed in HEK293 cells assessed as cAMP accumulation	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
	46885973	8120	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	490	4	1	3	5.0	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(Cl)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	CHEMBL1091632	8120	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	490	4	1	3	5.0	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccc(Cl)cc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
	44401319	12282	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1184826	12282	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028959	12282	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
	44393808	66131	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL184068	66131	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	44394079	126765	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	CHEMBL365278	126765	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
	137636965	156216	0	None	-5	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	CHEMBL4064433	156216	0	None	-5	4	Human	5.0	pEC50	=	5.0	Functional	Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF methodAgonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
	163196518	192129	2	None	-28	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	CHEMBL5203580	192129	2	None	-28	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysisAgonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
	145980719	166496	0	None	-5	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	CHEMBL4278563	166496	0	None	-5	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assayAgonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
	11353522	57182	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164884	57182	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	44401321	11796	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL1181867	11796	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	CHEMBL2028960	11796	0	None	19	2	Human	7.0	pEC50	=	7.0	Functional	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptorConcentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
	46884747	8395	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	CHEMBL1093306	8395	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulationAgonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
	11308184	64899	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL182231	64899	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Effective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptorEffective concentration against cAMP release in CHO cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
	CHEMBL410795	212842	0	None	-1	3	Human	6.0	pEC50	=	6.0	Functional	Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptorEffective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
	137656033	158643	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	CHEMBL4092477	158643	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assayAgonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay	ChEMBL	1034	20	15	16	-3.5	CSCC[C@H](NC(=O)[C@@H]1Cc2cn(nn2)C[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1)C(=O)O	10.1021/acs.jmedchem.7b00353
	122184638	122437	0	None	-18	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600919	122437	0	None	-18	4	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAgonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	49862737	15139	0	None	10	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	CHEMBL1209789	15139	0	None	10	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP releaseAgonist activity at human melanocortin 4 receptor expressed in CHO cells assessed as cAMP release	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
	137645483	157618	0	None	-2	3	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	906	11	11	10	-1.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	CHEMBL4081092	157618	0	None	-2	3	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assayAgonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay	ChEMBL	906	11	11	10	-1.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](CN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.6b01707
	44413592	78417	0	None	-1	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	CHEMBL211131	78417	0	None	-1	2	Human	5.0	pEC50	=	5.0	Functional	Activity at human MC4R by cAMP accumulation in SaoS2 cellsActivity at human MC4R by cAMP accumulation in SaoS2 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
	44394786	124080	0	None	-2	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	883	22	9	7	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	CHEMBL363271	124080	0	None	-2	3	Human	7.0	pEC50	=	7.0	Functional	Agonistic activity against human Melanocortin 4 receptorAgonistic activity against human Melanocortin 4 receptor	ChEMBL	883	22	9	7	3.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CCC(=O)c1cc(F)cc(F)c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2004.07.046
	90643842	111764	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	CHEMBL3287349	111764	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	ChEMBL	714	12	6	6	1.5	CC(=O)N1Cc2ccccc2CC1C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2CC1C(N)=O	10.1021/jm500064t
	46885861	8469	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	434	3	1	3	4.0	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	CHEMBL1093855	8469	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assayAgonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	ChEMBL	434	3	1	3	4.0	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
	5005059	24621	4	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	514	3	3	4	6.1	O=C1C2=C(N=C(S)NC2c2ccc(Cl)cc2)NC(c2ccc(Cl)cc2)N1c1ccc(Cl)cc1	nan
	CHEMBL1343101	24621	4	None	-3	2	Human	5.0	pEC50	=	5.0	Functional	PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: Luminescence-based cell-based high throughput dose response assay for biased ligands (agonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	514	3	3	4	6.1	O=C1C2=C(N=C(S)NC2c2ccc(Cl)cc2)NC(c2ccc(Cl)cc2)N1c1ccc(Cl)cc1	nan
	CHEMBL2323799	209525	0	None	-64	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N2C[C@H](CCCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	11845438	137623	0	None	5	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	CHEMBL375775	137623	0	None	5	3	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
	11490215	57154	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL164671	57154	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP releaseAgonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
	CHEMBL2323787	209513	0	None	-48	4	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assayAgonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)N2C[C@H](CCCNC(=N)N)NC(=O)[C@@H](CSCC2=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm301253y
	CHEMBL602650	215817	0	None	-2	3	Mouse	5.0	pEC50	=	5.0	Functional	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assayAgonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)NCC(=O)N(CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1016/j.bmc.2009.12.010
	11845804	79558	0	None	-123	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	CHEMBL211419	79558	0	None	-123	3	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human MC4R transfected in HEK293 cellsAgonist activity at human MC4R transfected in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
	71461643	78889	0	None	-194	2	Human	6.7	pED50	=	6.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	799	22	9	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	CHEMBL2112917	78889	0	None	-194	2	Human	6.7	pED50	=	6.7	Functional	Effective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulationEffective concentration against hMC4R using HEK293 cells was determined by measuring cAMP accumulation	ChEMBL	799	22	9	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
	3706223	59967	10	None	-	1	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	387	8	1	4	5.6	COc1ccccc1C1(CCNC(C)c2cccs2)CCOC(C(C)C)C1	nan
	CHEMBL1733168	59967	10	None	-	1	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	387	8	1	4	5.6	COc1ccccc1C1(CCNC(C)c2cccs2)CCOC(C(C)C)C1	nan
	9842665	156806	12	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4RAntagonist activity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
	CHEMBL40711	156806	12	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4RAntagonist activity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
	9842665	156806	12	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	2948635	36717	13	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	324	4	0	5	3.5	O=C1OCCC1Sc1nc2ccccc2n1Cc1ccccc1	nan
	CHEMBL1449356	36717	13	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	324	4	0	5	3.5	O=C1OCCC1Sc1nc2ccccc2n1Cc1ccccc1	nan
	CHEMBL3752534	212216	1	None	-213	4	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL3752534	212216	1	None	-213	4	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL267492	210724	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	16007285	81122	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	CHEMBL215659	81122	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	24687534	35623	6	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	519	8	2	8	2.7	CC(C)CN(C(=O)COC(=O)c1cnc(Cl)c(Cl)c1)c1c(N)n(Cc2ccccc2)c(=O)[nH]c1=O	nan
	CHEMBL1439680	35623	6	None	-	1	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	519	8	2	8	2.7	CC(C)CN(C(=O)COC(=O)c1cnc(Cl)c(Cl)c1)c1c(N)n(Cc2ccccc2)c(=O)[nH]c1=O	nan
	49792747	67393	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	479	11	1	7	4.0	CCc1nc2ccc(C(=O)NCc3ccc4c(c3)OCO4)cn2c1N(CCC(C)C)CCN(C)C	nan
	CHEMBL1887976	67393	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	479	11	1	7	4.0	CCc1nc2ccc(C(=O)NCc3ccc4c(c3)OCO4)cn2c1N(CCC(C)C)CCN(C)C	nan
	44202220	59916	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	437	5	1	5	4.7	COc1ccc2sc(-c3ccc(S(C)(=O)=O)cc3)c(-c3ccc(C(N)=O)cc3)c2c1	nan
	CHEMBL1731117	59916	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	437	5	1	5	4.7	COc1ccc2sc(-c3ccc(S(C)(=O)=O)cc3)c(-c3ccc(C(N)=O)cc3)c2c1	nan
	16437205	32003	9	None	2	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	486	6	1	7	2.7	CCC1CCCCN1S(=O)(=O)c1ccc(NC(=O)c2nc(S(C)(=O)=O)ncc2Cl)cc1	nan
	CHEMBL1407961	32003	9	None	2	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	486	6	1	7	2.7	CCC1CCCCN1S(=O)(=O)c1ccc(NC(=O)c2nc(S(C)(=O)=O)ncc2Cl)cc1	nan
	2140504	52836	20	None	1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	344	4	1	6	3.4	N#Cc1cc2c(nc1SCC(=O)Nc1nccs1)CCCCC2	nan
	CHEMBL1595336	52836	20	None	1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	344	4	1	6	3.4	N#Cc1cc2c(nc1SCC(=O)Nc1nccs1)CCCCC2	nan
	1080132	30271	9	None	1	4	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	4	1	5	2.5	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1	nan
	CHEMBL1391094	30271	9	None	1	4	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	4	1	5	2.5	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1	nan
	10077594	75590	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	CHEMBL204670	75590	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	CHEMBL267492	210724	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	5662106	22514	8	None	-1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	257	4	0	4	2.8	CN(C)c1ccc(-n2cccc2/C=C/[N+](=O)[O-])cc1	nan
	CHEMBL1325640	22514	8	None	-1	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	257	4	0	4	2.8	CN(C)c1ccc(-n2cccc2/C=C/[N+](=O)[O-])cc1	nan
	162674869	183314	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4797266	183314	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	1486292	34317	22	None	1	2	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	319	4	1	4	2.1	O=C1C=CC(=O)N1CCNc1ncc(C(F)(F)F)cc1Cl	nan
	CHEMBL1427185	34317	22	None	1	2	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	319	4	1	4	2.1	O=C1C=CC(=O)N1CCNc1ncc(C(F)(F)F)cc1Cl	nan
	162674869	183314	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4797266	183314	0	None	2	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1114	16	14	11	0.9	CC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	3761713	46237	6	None	-4	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	475	5	2	7	5.8	COc1ccc(OC)c(C2C3=C(O)CCCC3=NC(C)=C2C(=O)Nc2nc3ccccc3s2)c1	nan
	CHEMBL1534919	46237	6	None	-4	3	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	475	5	2	7	5.8	COc1ccc(OC)c(C2C3=C(O)CCCC3=NC(C)=C2C(=O)Nc2nc3ccccc3s2)c1	nan
	1316704	44939	6	None	9	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	0	3	4.8	C[S+]([O-])c1nc(-c2ccc(Br)cc2)cc(-c2ccccc2)c1C#N	nan
	CHEMBL1523206	44939	6	None	9	3	Human	5.9	pIC50	=	5.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	396	3	0	3	4.8	C[S+]([O-])c1nc(-c2ccc(Br)cc2)cc(-c2ccccc2)c1C#N	nan
	10324857	75992	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL205468	75992	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	44442997	93922	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	CHEMBL248205	93922	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
	16007264	79720	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	CHEMBL211564	79720	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP productionActivity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
	16007264	79720	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
	CHEMBL211564	79720	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
	CHEMBL267492	210724	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	1189526	27966	8	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	5	0	5	3.3	O=C(C[S+]([O-])c1ccc(C(F)(F)F)cc1[N+](=O)[O-])Oc1ccccc1	nan
	CHEMBL1372179	27966	8	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	5	0	5	3.3	O=C(C[S+]([O-])c1ccc(C(F)(F)F)cc1[N+](=O)[O-])Oc1ccccc1	nan
	392617	60220	2	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	378	17	0	0	7.9	CCCCCCCCCCCCCCCC[N+](C)(C)Cc1ccc(F)cc1	nan
	CHEMBL1717770	60220	2	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	378	17	0	0	7.9	CCCCCCCCCCCCCCCC[N+](C)(C)Cc1ccc(F)cc1	nan
	CHEMBL1740201	60220	2	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	378	17	0	0	7.9	CCCCCCCCCCCCCCCC[N+](C)(C)Cc1ccc(F)cc1	nan
	CHEMBL1724806	59746	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL		None	None	None		None	nan
	2126229	34391	6	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	360	7	1	7	1.6	Cc1ccc(CNC(=O)COC(=O)Cn2nc(C)c([N+](=O)[O-])c2C)cc1	nan
	CHEMBL1427945	34391	6	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	360	7	1	7	1.6	Cc1ccc(CNC(=O)COC(=O)Cn2nc(C)c([N+](=O)[O-])c2C)cc1	nan
	44577093	178646	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL467587	178646	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	44577094	178647	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL467588	178647	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	10050686	76016	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	CHEMBL205553	76016	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
	44447849	155466	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL403938	155466	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
	21773133	72853	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	460	3	1	6	4.5	CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	CHEMBL2002430	72853	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	460	3	1	6	4.5	CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	2713	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5353524	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5360566	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	88536661	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	9552079	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL1330113	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL790	205271	82	None	-1	27	Human	5.8	pIC50	=	5.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	1831123	20849	8	None	-1	3	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	489	3	1	7	5.2	Cc1nc2c(sc3nc(N4CCOCC4)c4c(c32)CC(C)(C)OC4)c(-c2ccccc2)c1C(=O)O	nan
	CHEMBL1310276	20849	8	None	-1	3	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	489	3	1	7	5.2	Cc1nc2c(sc3nc(N4CCOCC4)c4c(c32)CC(C)(C)OC4)c(-c2ccccc2)c1C(=O)O	nan
	CHEMBL267492	210724	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAntagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	162673931	183058	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794168	183058	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44577063	188100	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL498150	188100	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	24740653	88592	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	CHEMBL235556	88592	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	9842665	156806	12	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	162667953	182537	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787322	182537	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	162673931	183058	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794168	183058	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL267492	210724	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	101176453	182962	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4792986	182962	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	44410379	141203	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
	CHEMBL382833	141203	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
	24741624	138380	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
	CHEMBL377231	138380	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
	24741624	138380	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
	CHEMBL377231	138380	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
	10031074	76343	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
	CHEMBL205898	76343	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
	162667953	182537	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4787322	182537	0	None	2	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	15	12	10	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/acs.jmedchem.0c01620
	44246589	59261	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	13	2	5	5.3	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1C(C)C)N1C[C@@H](Cc2ccccc2)N(CCCC2CCCC2)C1=N	nan
	CHEMBL1703869	59261	0	None	-	1	Human	4.8	pIC50	=	4.8	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	13	2	5	5.3	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1C(C)C)N1C[C@@H](Cc2ccccc2)N(CCCC2CCCC2)C1=N	nan
	101176453	182962	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4792986	182962	0	None	-245	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1034	15	12	10	0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL267492	210724	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	44410188	140380	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
	CHEMBL380854	140380	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
	44410385	139854	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
	CHEMBL379918	139854	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
	44433446	151964	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL396660	151964	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	3957801	59302	28	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	203	2	1	5	1.9	CCOC(=O)c1sc(S)nc1C	nan
	CHEMBL1705379	59302	28	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	203	2	1	5	1.9	CCOC(=O)c1sc(S)nc1C	nan
	24740655	89086	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	CHEMBL236521	89086	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
	24740655	89086	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
	CHEMBL236521	89086	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
	44447804	155594	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL404503	155594	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	23635108	144963	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	CHEMBL391056	144963	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	23635108	144963	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL391056	144963	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	1190554	42923	12	None	-3	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	5	1	6	4.3	CCOC(=O)c1cnc2ccc(C)cc2c1Nc1ccc(N2CCOCC2)cc1	nan
	CHEMBL1503392	42923	12	None	-3	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	391	5	1	6	4.3	CCOC(=O)c1cnc2ccc(C)cc2c1Nc1ccc(N2CCOCC2)cc1	nan
	49778648	66990	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	429	8	1	7	3.7	c1ccc(COc2ccc(-c3cc4nc(NCCN5CCOCC5)ccn4n3)cc2)cc1	nan
	CHEMBL1868672	66990	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	429	8	1	7	3.7	c1ccc(COc2ccc(-c3cc4nc(NCCN5CCOCC5)ccn4n3)cc2)cc1	nan
	2713	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5353524	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	5360566	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	88536661	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	9552079	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL1330113	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	CHEMBL790	205271	82	None	-1	27	Human	5.7	pIC50	=	5.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	nan
	10855168	181906	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4779301	181906	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	10855168	181906	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4779301	181906	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1050	15	13	11	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/acs.jmedchem.0c01620
	1326639	34883	10	None	-1	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	4	1	4	3.7	O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1	nan
	CHEMBL1431891	34883	10	None	-1	3	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	373	4	1	4	3.7	O=C(Nc1ccccc1C(=O)N1CCCC1)c1ccc(Cl)c([N+](=O)[O-])c1	nan
	24180646	148182	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
	CHEMBL393576	148182	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
	24180646	148182	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL393576	148182	0	None	3	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	44434568	89176	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
	CHEMBL236650	89176	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
	CHEMBL267492	210724	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	44433262	146073	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL391914	146073	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	46902089	72923	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	5	2	7	4.3	CC(O)CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	CHEMBL2004734	72923	0	None	-	1	Human	4.7	pIC50	=	4.7	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	504	5	2	7	4.3	CC(O)CC(=O)OC[C@]12CC[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1CC(C1=CC(=O)OC1O)O2	nan
	44202417	59759	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	643	8	4	6	5.7	COc1ccc(NC(=O)Nc2cccc3c2O[C@H](CN(C)C(=O)Nc2ccc(C(F)(F)F)cc2)[C@@H](C)CN([C@H](C)CO)C3=O)cc1	nan
	CHEMBL1725374	59759	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	643	8	4	6	5.7	COc1ccc(NC(=O)Nc2cccc3c2O[C@H](CN(C)C(=O)Nc2ccc(C(F)(F)F)cc2)[C@@H](C)CN([C@H](C)CO)C3=O)cc1	nan
	44447847	155432	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL403749	155432	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	23635105	154979	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
	CHEMBL401250	154979	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
	23635105	154979	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL401250	154979	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
	17573520	55992	4	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	470	13	0	1	9.2	CCCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1548086	55992	4	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	470	13	0	1	9.2	CCCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1624390	55992	4	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	470	13	0	1	9.2	CCCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL267492	210724	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	25211670	174260	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL454916	174260	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	44562460	189265	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL511826	189265	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	2998271	37846	9	None	1	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	5	2	5	4.1	CC(C)(C)c1cc(C(c2cccnc2)N2CCN(CCO)CC2)cc(C(C)(C)C)c1O	nan
	CHEMBL1458840	37846	9	None	1	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	5	2	5	4.1	CC(C)(C)c1cc(C(c2cccnc2)N2CCN(CCO)CC2)cc(C(C)(C)C)c1O	nan
	3216692	55648	2	None	5	2	Human	5.6	pIC50	=	5.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	412	7	1	5	3.5	C#CC(=O)N(c1ccc(OC)c(OC)c1)C(C(=O)NC1CCCC1)c1cccs1	nan
	CHEMBL1458479	55648	2	None	5	2	Human	5.6	pIC50	=	5.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	412	7	1	5	3.5	C#CC(=O)N(c1ccc(OC)c(OC)c1)C(C(=O)NC1CCCC1)c1cccs1	nan
	CHEMBL1621541	55648	2	None	5	2	Human	5.6	pIC50	=	5.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	412	7	1	5	3.5	C#CC(=O)N(c1ccc(OC)c(OC)c1)C(C(=O)NC1CCCC1)c1cccs1	nan
	44410207	161759	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
	CHEMBL413931	161759	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
	10481883	77335	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL208376	77335	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	10325306	141264	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL383117	141264	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	25058412	189440	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL513404	189440	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	44825857	66939	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	331	3	0	6	2.9	COc1ccc(CN2Cc3cnnn3-c3ccccc3C2C#N)cc1	nan
	CHEMBL1866397	66939	0	None	-	1	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	331	3	0	6	2.9	COc1ccc(CN2Cc3cnnn3-c3ccccc3C2C#N)cc1	nan
	135419062	27457	6	None	-1	2	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	431	5	1	7	4.5	N#Cc1c(O)nc(SCC(=O)c2ccc(Br)cc2)nc1-c1cccs1	nan
	CHEMBL1368444	27457	6	None	-1	2	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	431	5	1	7	4.5	N#Cc1c(O)nc(SCC(=O)c2ccc(Br)cc2)nc1-c1cccs1	nan
	2371253	28608	5	None	-5	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	458	7	1	6	4.5	O=C(COC(=O)c1ccccc1C(=O)c1ccc(Cl)c([N+](=O)[O-])c1)NC1CCCCCC1	nan
	CHEMBL1376861	28608	5	None	-5	3	Human	4.6	pIC50	=	4.6	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	458	7	1	6	4.5	O=C(COC(=O)c1ccccc1C(=O)c1ccc(Cl)c([N+](=O)[O-])c1)NC1CCCCCC1	nan
	44577060	188052	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL497746	188052	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	9842665	156806	12	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	23635237	91453	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
	CHEMBL240364	91453	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
	23635237	91453	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL240364	91453	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
	9842665	156806	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	44577092	178645	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL467586	178645	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	9842665	156806	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	3573522	28756	16	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	374	3	1	5	4.6	CC1(C)CC(=O)C(C(C2=C(O)CC(C)(C)CC2=O)c2cccs2)C(=O)C1	nan
	CHEMBL1378309	28756	16	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	374	3	1	5	4.6	CC1(C)CC(=O)C(C(C2=C(O)CC(C)(C)CC2=O)c2cccs2)C(=O)C1	nan
	CHEMBL2370964	209967	0	None	-74	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	CHEMBL2370964	209967	0	None	-74	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	CHEMBL2370968	209971	0	None	-6	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	44577062	193374	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL525177	193374	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	4113455	72681	12	None	-1	2	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	463	4	1	6	4.1	C=CCn1/c(=N/C(=O)c2sc3ccccc3c2Cl)sc2cc(S(N)(=O)=O)ccc21	nan
	CHEMBL1996519	72681	12	None	-1	2	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	463	4	1	6	4.1	C=CCn1/c(=N/C(=O)c2sc3ccccc3c2Cl)sc2cc(S(N)(=O)=O)ccc21	nan
	44410175	168992	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL439158	168992	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
	44447773	95706	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL258245	95706	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	1846364	56092	5	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	456	12	0	1	8.8	CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1589425	56092	5	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	456	12	0	1	8.8	CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	CHEMBL1625287	56092	5	None	-	1	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	456	12	0	1	8.8	CCCCCCCCCC[N+](C)(C)CC/C=C1/c2ccccc2Sc2ccc(Cl)cc21	nan
	162672837	183021	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793821	183021	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162672837	183021	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793821	183021	0	None	17	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	10369375	77218	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL207946	77218	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	44577090	178666	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL467771	178666	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	44433283	96460	1	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL262320	96460	1	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	23635235	166501	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	CHEMBL427860	166501	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	23635235	166501	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL427860	166501	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	44433297	153046	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397582	153046	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162676295	183453	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4798971	183453	0	None	2	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	101043845	190392	1	None	4	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL5177536	190392	1	None	4	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	9842665	156806	12	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	1002526	41115	11	None	-5	3	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	371	2	1	4	4.1	O=C(O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(Br)cc12	nan
	CHEMBL1488092	41115	11	None	-5	3	Human	4.5	pIC50	=	4.5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	371	2	1	4	4.1	O=C(O)c1cc(-c2ccc3c(c2)OCO3)nc2ccc(Br)cc12	nan
	162676295	183453	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4798971	183453	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433264	89351	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL236940	89351	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162673650	183053	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794121	183053	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162673650	183053	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794121	183053	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	759209	35971	10	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	259	1	0	3	3.5	Cc1c(Cl)sn(-c2ccc(Cl)cc2)c1=O	nan
	CHEMBL1442788	35971	10	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	259	1	0	3	3.5	Cc1c(Cl)sn(-c2ccc(Cl)cc2)c1=O	nan
	9842665	156806	12	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	1325	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	6440621	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	9898183	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	CHEMBL3422426	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	1325	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	6440621	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	9898183	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	CHEMBL3422426	3600	14	None	-57	5	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
	162668987	182590	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4788071	182590	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	2839884	45481	35	None	-	1	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	4	1	12	4.0	COC(=O)C1=C(C(=O)OC)SC2(S1)C(C(=O)OC)=C(C(=O)OC)SC1=C2c2cccc(C)c2NC1(C)C	nan
	CHEMBL1528149	45481	35	None	-	1	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	563	4	1	12	4.0	COC(=O)C1=C(C(=O)OC)SC2(S1)C(C(=O)OC)=C(C(=O)OC)SC1=C2c2cccc(C)c2NC1(C)C	nan
	4096875	59403	1	None	-	1	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	9	2	5	2.9	O=C(COC(=O)C(Cc1ccccc1)NC(=O)c1cccs1)NCc1ccccc1	nan
	CHEMBL1709842	59403	1	None	-	1	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	422	9	2	5	2.9	O=C(COC(=O)C(Cc1ccccc1)NC(=O)c1cccs1)NCc1ccccc1	nan
	162668987	182590	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4788071	182590	0	None	6	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44410041	141265	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
	CHEMBL383120	141265	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
	44577091	178667	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL467772	178667	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	162675203	183261	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4796506	183261	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162675203	183261	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4796506	183261	0	None	10	2	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1122	16	14	11	1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=N)N)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL2370968	209971	0	None	-6	4	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/acs.jmedchem.1c01295
	162677173	183528	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799891	183528	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44562287	174248	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL454900	174248	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
	162677173	183528	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799891	183528	0	None	2	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1088	18	14	11	0.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	23635107	91558	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	CHEMBL240571	91558	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	44442981	153078	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	CHEMBL397608	153078	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
	23635107	91558	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL240571	91558	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	44577061	192641	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL521715	192641	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
	44562440	179041	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL471340	179041	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
	1050448	41639	14	None	-4	2	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	385	4	0	4	5.6	COc1cc(-c2nc3ccc4ccccc4c3c3c2CCC3)cc(OC)c1OC	nan
	CHEMBL1491876	41639	14	None	-4	2	Human	4.4	pIC50	=	4.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	385	4	0	4	5.6	COc1cc(-c2nc3ccc4ccccc4c3c3c2CCC3)cc(OC)c1OC	nan
	24180593	148443	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL393788	148443	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	216239	23795	118	None	-2	11	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	464	5	3	4	5.6	CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1	nan
	CHEMBL1200485	23795	118	None	-2	11	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	464	5	3	4	5.6	CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1	nan
	CHEMBL1336	23795	118	None	-2	11	Human	5.4	pIC50	=	5.4	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	464	5	3	4	5.6	CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1	nan
	9983075	77308	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL208268	77308	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
	44433279	151709	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL396433	151709	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162673640	182982	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793346	182982	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44443035	154417	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	CHEMBL398929	154417	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
	44433272	147712	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL393204	147712	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162673640	182982	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4793346	182982	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44577089	178747	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL468579	178747	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	44577064	187917	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL496710	187917	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	44433294	153043	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397580	153043	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	24740419	148194	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
	CHEMBL393584	148194	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
	CHEMBL267492	210724	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	162643518	181711	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776915	181711	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162643518	181711	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4776915	181711	0	None	102	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	1482612	25250	16	None	-	1	Human	5.3	pIC50	=	5.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	407	3	1	5	5.0	O=C(O)c1cnn(-c2nc(-c3ccc(Cl)c(Cl)c3)cs2)c1C(F)(F)F	nan
	CHEMBL1348506	25250	16	None	-	1	Human	5.3	pIC50	=	5.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	407	3	1	5	5.0	O=C(O)c1cnn(-c2nc(-c3ccc(Cl)c(Cl)c3)cs2)c1C(F)(F)F	nan
	23661656	169044	0	None	7	2	Human	6.3	pIC50	=	6.3	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
	CHEMBL439560	169044	0	None	7	2	Human	6.3	pIC50	=	6.3	Functional	Agonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP productionAgonist activity at human MC4 receptor in HEK293 cells assessed as inhibition of alpha-MSH stimulated cAMP production	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
	44433298	153047	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397583	153047	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162672763	183124	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794990	183124	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44447777	155415	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL403675	155415	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	162664942	182193	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4782808	182193	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162664942	182193	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4782808	182193	0	None	2	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1158	16	14	11	1.3	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433285	88616	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL235640	88616	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	162672763	183124	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4794990	183124	0	None	6	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	10075878	75991	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	CHEMBL205461	75991	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
	44447250	94727	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
	CHEMBL253028	94727	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
	1343565	38861	9	None	-	1	Human	4.3	pIC50	=	4.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	2	6	3.8	Cc1ccc(-n2nc3ccc(NC(=S)NC(=O)/C=C/c4ccco4)cc3n2)cc1	nan
	CHEMBL1467018	38861	9	None	-	1	Human	4.3	pIC50	=	4.3	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	2	6	3.8	Cc1ccc(-n2nc3ccc(NC(=S)NC(=O)/C=C/c4ccco4)cc3n2)cc1	nan
	16046215	80089	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
	CHEMBL213122	80089	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Activity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cellsActivity at MC4R assessed as inhibition of alpha MSH-stimulated cAMP production in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
	44455922	155136	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
	CHEMBL402075	155136	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
	9842665	156806	12	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAntagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulationAntagonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	101043845	190392	1	None	4	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	CHEMBL5177536	190392	1	None	4	2	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assayAntagonist activity at human MC4R transfected in HEK293 cells co-transfected with GScAMP22F assessed as decrease in alpha-MSH induced cAMP level in presence of 70 nM alpha-MSH by split luciferase cAMP sensor dynamic assay	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.1c01295
	16046215	80089	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
	CHEMBL213122	80089	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
	10414731	76548	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL206141	76548	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
	874744	41405	8	None	-	1	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	269	3	1	2	3.9	C=C1CCc2c([nH]c3ccc(OCC(C)C)cc23)C1=O	nan
	CHEMBL1490308	41405	8	None	-	1	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	269	3	1	2	3.9	C=C1CCc2c([nH]c3ccc(OCC(C)C)cc23)C1=O	nan
	9842665	156806	12	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I125L expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	28777	46014	80	None	-	1	Human	4.2	pIC50	=	4.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	261	2	0	3	3.3	O=C1c2ccccc2C(=O)N1SC1CCCCC1	nan
	CHEMBL1532794	46014	80	None	-	1	Human	4.2	pIC50	=	4.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	261	2	0	3	3.3	O=C1c2ccccc2C(=O)N1SC1CCCCC1	nan
	448949	120792	89	None	-5	3	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	355	2	3	3	5.2	O=Nc1c(-c2c(O)[nH]c3cc(Br)ccc23)[nH]c2ccccc12	nan
	CHEMBL355496	120792	89	None	-5	3	Human	5.2	pIC50	=	5.2	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	355	2	3	3	5.2	O=Nc1c(-c2c(O)[nH]c3cc(Br)ccc23)[nH]c2ccccc12	nan
	44456219	155438	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	CHEMBL403806	155438	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
	162643092	181724	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4777048	181724	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44447785	95077	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL255313	95077	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	44433439	89924	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	CHEMBL237976	89924	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISAAntagonist activity at human MC4 receptor expressed in CHO cells assessed as inhibition of alpha-MSH-stimulated of cAMP production by ELISA	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
	162643092	181724	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4777048	181724	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44410046	75951	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
	CHEMBL205214	75951	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
	44562414	176817	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	CHEMBL460942	176817	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
	162665567	182349	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784635	182349	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	44410378	76626	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
	CHEMBL206367	76626	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
	23635106	91557	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	CHEMBL240568	91557	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
	23635106	91557	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL240568	91557	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	162665567	182349	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4784635	182349	0	None	4	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	11756904	76586	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
	CHEMBL206316	76586	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
	44447221	94669	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
	CHEMBL252584	94669	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assayAntagonist activity at human MC4R assessed as inhibition of alpha MSH-stimulated cAMP release by cell based assay	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
	44410040	76518	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	CHEMBL205996	76518	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
	9842665	156806	12	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	CHEMBL40711	156806	12	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
	44143139	59768	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	673	13	2	5	6.4	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@@H]1Cc1ccccc1)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	CHEMBL1725591	59768	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	673	13	2	5	6.4	CC(C)[C@H](CN1CCC[C@H]1CN1C(N)=NC[C@@H]1Cc1ccccc1)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	44447780	95044	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL255100	95044	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
	44825858	67454	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	315	2	0	5	3.2	Cc1ccccc1CN1Cc2cnnn2-c2ccccc2C1C#N	nan
	CHEMBL1891068	67454	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	315	2	0	5	3.2	Cc1ccccc1CN1Cc2cnnn2-c2ccccc2C1C#N	nan
	3617229	44502	7	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	394	4	2	4	5.4	O=C(Nc1ccccc1)OC1CCC2CC1CCC2OC(=O)Nc1ccccc1	nan
	CHEMBL1519347	44502	7	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	394	4	2	4	5.4	O=C(Nc1ccccc1)OC1CCC2CC1CCC2OC(=O)Nc1ccccc1	nan
	44577055	193296	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	CHEMBL524060	193296	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
	1336753	30164	14	None	-7	4	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	1	6	3.9	O=[N+]([O-])c1cc(S(=O)(=O)C(F)(F)F)ccc1Sc1nc2ccccc2[nH]1	nan
	CHEMBL1390139	30164	14	None	-7	4	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	403	4	1	6	3.9	O=[N+]([O-])c1cc(S(=O)(=O)C(F)(F)F)ccc1Sc1nc2ccccc2[nH]1	nan
	44246581	30672	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	639	14	2	5	6.4	CCC[C@@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1CC(C)C)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	CHEMBL1394750	30672	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	639	14	2	5	6.4	CCC[C@@H](CN1CCC[C@H]1CN1C(N)=NC[C@H]1CC(C)C)N1C[C@@H](Cc2ccccc2)N(CCc2ccc(Cl)c(Cl)c2)C1=N	nan
	162644475	181805	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4778074	181805	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	162644475	181805	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4778074	181805	0	None	2	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1110	16	12	10	2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](c3ccccc3)CN2C1=O	10.1021/acs.jmedchem.0c01620
	162677133	183557	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4800268	183557	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162677133	183557	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4800268	183557	0	None	9	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	42628546	59846	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	382	8	0	2	5.6	CCCCCCCN(c1ccccc1)[C@H]1C[C@@H]2CCN3C(=O)CCC[C@H](C1)[C@H]23	nan
	CHEMBL1728670	59846	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	382	8	0	2	5.6	CCCCCCCN(c1ccccc1)[C@H]1C[C@@H]2CCN3C(=O)CCC[C@H](C1)[C@H]23	nan
	CHEMBL267492	210724	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulationAntagonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
	44433299	153048	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL397584	153048	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	5291838	42689	10	None	3	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	287	2	0	4	3.9	CC1=NOC(=O)/C1=C/c1ccc(-c2ccc(Cl)cc2)o1	nan
	CHEMBL1501376	42689	10	None	3	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	287	2	0	4	3.9	CC1=NOC(=O)/C1=C/c1ccc(-c2ccc(Cl)cc2)o1	nan
	2575495	45783	6	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	534	9	2	6	4.1	O=C(COC(=O)CNS(=O)(=O)c1cccc(Br)c1)Nc1ccccc1Sc1ccccc1	nan
	CHEMBL1530780	45783	6	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	534	9	2	6	4.1	O=C(COC(=O)CNS(=O)(=O)c1cccc(Br)c1)Nc1ccccc1Sc1ccccc1	nan
	1335691	25549	5	None	1	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	4	1	5	3.2	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1Cl	nan
	CHEMBL1351081	25549	5	None	1	2	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	425	4	1	5	3.2	Cc1ccc(NC(=O)c2cc(N3C(=O)C=CC3=O)ccc2N2CCOCC2)cc1Cl	nan
	10049407	77330	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
	CHEMBL208366	77330	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
	1190175	19588	9	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	449	7	1	8	4.2	CCOC(=O)c1ccc2ncc(C(=O)OCC)c(Nc3ccc(N4CCOCC4)cc3)c2c1	nan
	CHEMBL1300063	19588	9	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	449	7	1	8	4.2	CCOC(=O)c1ccc2ncc(C(=O)OCC)c(Nc3ccc(N4CCOCC4)cc3)c2c1	nan
	23635236	91601	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
	CHEMBL240780	91601	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
	23635236	91601	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	CHEMBL240780	91601	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
	362664	60175	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	313	7	0	2	4.5	CC(C)Cc1ccc(C(C)CC2=CCC(CN(C)C)C2=O)cc1	nan
	CHEMBL1699592	60175	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	313	7	0	2	4.5	CC(C)Cc1ccc(C(C)CC2=CCC(CN(C)C)C2=O)cc1	nan
	CHEMBL1739768	60175	2	None	-	1	Human	5.1	pIC50	=	5.1	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	313	7	0	2	4.5	CC(C)Cc1ccc(C(C)CC2=CCC(CN(C)C)C2=O)cc1	nan
	23635109	91559	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	CHEMBL240572	91559	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP releaseAntagonist activity at MC4R assessed as inhibition of alpha-MSH-stimulated cAMP release	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
	23635109	91559	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	CHEMBL240572	91559	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISAAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of alpha-MSH-induced cAMP production by ELISA	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
	44447804	155594	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	CHEMBL404503	155594	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
	24180592	97013	0	None	-1	2	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
	CHEMBL266647	97013	0	None	-1	2	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4R expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
	44601668	59131	0	None	2	2	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	428	4	1	3	5.6	O=S(=O)(/C(=C\c1ccc(C(F)(F)F)cc1)c1nc2ccccc2[nH]1)c1ccccc1	nan
	CHEMBL1698464	59131	0	None	2	2	Human	5.0	pIC50	=	5.0	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	428	4	1	3	5.6	O=S(=O)(/C(=C\c1ccc(C(F)(F)F)cc1)c1nc2ccccc2[nH]1)c1ccccc1	nan
	44433293	144923	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	CHEMBL391028	144923	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
	44447851	94936	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	CHEMBL254364	94936	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at MC4 receptor assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2NCC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
	44410176	76024	7	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
	CHEMBL205594	76024	7	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity against MC4R by cAMP functional assayAntagonist activity against MC4R by cAMP functional assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
	162675582	183460	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799036	183460	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	162675582	183460	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	CHEMBL4799036	183460	0	None	5	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assayAntagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay	ChEMBL	1108	16	14	11	0.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
	44433271	89539	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
	CHEMBL237365	89539	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assayAntagonist activity at human MC4R expressed in HEK293 cells by cAMP accumulation assay	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
	1472220	41895	11	None	-4	3	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	418	6	1	4	4.3	COc1ccc(NC(=O)/C(Cl)=C(/Cl)[S+]([O-])Cc2ccc(Cl)cc2)cn1	nan
	CHEMBL1494120	41895	11	None	-4	3	Human	5.0	pIC50	=	5	Functional	PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory) PUBCHEM_BIOASSAY: TRFRET-based cell-based high throughput dose response assay for biased ligands (antagonists) of the melanocortin 4 receptor (MC4R). (Class of assay: confirmatory)	ChEMBL	418	6	1	4	4.3	COc1ccc(NC(=O)/C(Cl)=C(/Cl)[S+]([O-])Cc2ccc(Cl)cc2)cn1	nan
	CHEMBL428801	213472	0	None	-21	5	Human	9.7	pKd	=	9.7	Functional	Evaluated for partial agonistic activity at cloned mammalian Melanocortin 4 receptorEvaluated for partial agonistic activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	145953129	162440	0	None	-	0	Mouse	9.6	pKd	=	9.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1001	16	13	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4166449	162440	0	None	-	0	Mouse	9.6	pKd	=	9.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1001	16	13	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145957551	162264	0	None	-	1	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1015	17	13	11	-1.5	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4163787	162264	0	None	-	1	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1015	17	13	11	-1.5	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145960041	162286	0	None	-	0	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	945	14	11	11	-1.8	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4164111	162286	0	None	-	0	Mouse	9.5	pKd	=	9.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	945	14	11	11	-1.8	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	127035019	136436	0	None	-	1	Mouse	9.3	pKd	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	136436	0	None	-	1	Mouse	9.3	pKd	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL266417	210683	0	None	-50	6	Human	9.3	pKd	=	9.3	Functional	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptorEvaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
	145952883	162415	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	973	15	11	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4166050	162415	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	973	15	11	11	-1.9	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145951686	162956	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	979	13	11	11	-1.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4174761	162956	0	None	-	0	Mouse	9.2	pKd	=	9.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	979	13	11	11	-1.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL2096742	209206	0	None	-1	6	Human	9.1	pKd	=	9.1	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulationAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT2 induced intracellular cAMP accumulation	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm070461w
	137655051	158966	0	None	-	0	Human	9.1	pKd	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4096081	158966	0	None	-	0	Human	9.1	pKd	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	127035019	136436	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	136436	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	145956526	162192	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	929	13	10	10	-0.8	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4162603	162192	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	929	13	10	10	-0.8	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145958585	162339	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	931	13	11	11	-2.2	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4164846	162339	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	931	13	11	11	-2.2	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145954663	162657	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	985	15	12	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4169872	162657	0	None	-	0	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	985	15	12	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145950765	162833	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	964	12	11	11	-2.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4172753	162833	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	964	12	11	11	-2.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	145951839	162875	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4173301	162875	0	None	-	1	Mouse	9.1	pKd	=	9.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	162650385	180071	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4747952	180071	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	145957356	161988	0	None	-	0	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1035	15	13	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4159229	161988	0	None	-	0	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1035	15	13	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	145954673	162671	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	915	12	10	10	-1.2	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4170160	162671	0	None	-	1	Mouse	9.0	pKd	=	9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	915	12	10	10	-1.2	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145951083	162976	0	None	-	0	Mouse	8.9	pKd	=	8.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1033	15	12	10	-0.4	C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4175108	162976	0	None	-	0	Mouse	8.9	pKd	=	8.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1033	15	12	10	-0.4	C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	145952946	162485	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	999	16	12	10	-0.5	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4167239	162485	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	999	16	12	10	-0.5	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145949639	162757	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1049	16	13	11	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4171666	162757	0	None	-	0	Mouse	8.8	pKd	=	8.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1049	16	13	11	-1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	10.1021/acs.jmedchem.8b00684
	132938008	159513	0	None	3	5	Mouse	8.7	pKd	=	8.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4102048	159513	0	None	3	5	Mouse	8.7	pKd	=	8.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	122184635	122434	0	None	-56	4	Human	8.0	pKd	=	8	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	CHEMBL3600916	122434	0	None	-56	4	Human	8.0	pKd	=	8	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence countingAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
	127046262	139820	0	None	23	3	Mouse	8.0	pKd	=	8.0	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3798912	139820	0	None	23	3	Mouse	8.0	pKd	=	8.0	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	132180597	156171	0	None	-117	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4063911	156171	0	None	-117	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155542149	173092	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	740	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4520119	173092	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	740	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155544214	173331	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	797	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4526652	173331	0	None	-	3	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	797	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155563222	175291	0	None	-524	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4572994	175291	0	None	-524	4	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	711	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	137662060	159205	0	None	-	1	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	991	13	10	10	-0.2	C[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4098651	159205	0	None	-	1	Mouse	7.0	pKd	=	7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	991	13	10	10	-0.2	C[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137659091	159340	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4100160	159340	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	806	12	6	6	1.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	137657151	159556	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4102613	159556	0	None	-	3	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	155546131	173530	0	None	2	5	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4531291	173530	0	None	2	5	Mouse	6.0	pKd	=	6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	162664463	182190	0	None	-	3	Mouse	5.0	pKd	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4782762	182190	0	None	-	3	Mouse	5.0	pKd	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL2370694	209911	0	None	-	1	Mouse	7.0	pKd	=	7.0	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	6918814	127057	1	None	-	0	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	CHEMBL365597	127057	1	None	-	0	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP productionAntagonist activity at human MC4 receptor expressed in HEK293 cells assessed as inhibition of alpha-MSH-stimulated cAMP production	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
	137642804	158371	0	None	-	1	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4089759	158371	0	None	-	1	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	132180653	175059	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4567961	175059	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	137641768	158106	0	None	-	0	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	13	9	9	1.1	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4086679	158106	0	None	-	0	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	13	9	9	1.1	CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	162673830	183159	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4795352	183159	0	None	-	3	Mouse	6.9	pKd	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	137635892	155905	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4060738	155905	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137633477	156595	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4068777	156595	0	None	-	1	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137643799	158438	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4090448	158438	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	155556047	174497	0	None	-199	4	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4554828	174497	0	None	-199	4	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	683	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	137654977	158806	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	11	9	9	0.6	CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4094419	158806	0	None	-	0	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	11	9	9	0.6	CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	155536962	172237	0	None	10	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4474215	172237	0	None	10	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	162672755	183090	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4794484	183090	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 6 hrs by beta-galactosidase cAMP assay	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	164610489	184555	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	600	10	4	4	5.8	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4848322	184555	0	None	-	3	Mouse	5.9	pKd	=	5.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	600	10	4	4	5.8	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL2370695	209912	0	None	-1	2	Mouse	5.9	pKd	=	5.9	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	127046262	139820	0	None	-	3	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798912	139820	0	None	-	3	Human	7.9	pKd	=	7.9	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL2370696	209913	0	None	-	1	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCNC(=O)C[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	CHEMBL103817	208459	0	None	-	4	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	127047336	139798	0	None	-	4	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3798768	139798	0	None	-	4	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
	155548853	173809	0	None	-6	5	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4538274	173809	0	None	-6	5	Human	7.8	pKd	=	7.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	132180598	157849	0	None	-25	4	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4083717	157849	0	None	-25	4	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL407346	212656	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	137632506	156524	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1049	12	10	9	1.6	C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4067947	156524	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1049	12	10	9	1.6	C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	145955736	162553	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1331	22	17	17	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(N)=O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4168324	162553	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1331	22	17	17	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N[C@@H](Cc2ccc(O)cc2)C(N)=O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	155555217	174337	0	None	-812	4	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4550976	174337	0	None	-812	4	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162649653	180100	0	None	-	3	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4748317	180100	0	None	-	3	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL2096710	209205	0	None	-53	3	Mouse	6.8	pKd	=	6.8	Functional	Antagonistic activity against mouse Melanocortin 4 ReceptorAntagonistic activity against mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049620r
	44310372	158581	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1436	23	17	21	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CSSSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	91932915	158581	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1436	23	17	21	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CSSSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	CHEMBL409190	158581	0	None	-	1	Mouse	6.8	pKd	=	6.8	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	1436	23	17	21	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CSSSSC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
	155536962	172237	0	None	-10	3	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4474215	172237	0	None	-10	3	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155566718	175916	0	None	-3	2	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4587214	175916	0	None	-3	2	Human	5.8	pKd	=	5.8	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	137657385	159766	0	None	-	1	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	867	21	11	7	0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4105142	159766	0	None	-	1	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	867	21	11	7	0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	164609130	184427	0	None	-	3	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	595	10	4	4	5.1	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4846261	184427	0	None	-	3	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	595	10	4	4	5.1	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	164621263	185482	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	598	11	3	3	7.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1	10.1021/acs.jmedchem.0c02041
	CHEMBL4862172	185482	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	598	11	3	3	7.2	CCC[C@@H]1CN([C@H](CC2CCCCC2)N2CCC[C@H]2CN2C(=N)NC[C@H]2C(C)C)C(=N)N1CC1CCC(C(C)(C)C)CC1	10.1021/acs.jmedchem.0c02041
	164624627	185879	0	None	-3	4	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4868223	185879	0	None	-3	4	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	589	10	4	4	4.4	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	164627764	186564	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	603	11	4	4	4.8	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4878201	186564	0	None	-	2	Mouse	5.8	pKd	=	5.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	603	11	4	4	4.8	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC23CC4CC(CC(C4)C2)C3)C1=N	10.1021/acs.jmedchem.0c02041
	137653029	158715	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	977	12	10	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4093379	158715	0	None	-	0	Mouse	6.8	pKd	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	977	12	10	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137639030	156945	0	None	-	0	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	963	11	10	10	-0.7	C[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4072662	156945	0	None	-	0	Mouse	7.8	pKd	=	7.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	963	11	10	10	-0.7	C[C@@H]1NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137659851	159437	0	None	-	0	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	949	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4101128	159437	0	None	-	0	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	949	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137654791	158918	0	None	-	0	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1053	14	10	10	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4095539	158918	0	None	-	0	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1053	14	10	10	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137659513	159250	0	None	-	1	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4099096	159250	0	None	-	1	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	882	18	8	6	3.3	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	155553683	174183	0	None	-295	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4547556	174183	0	None	-295	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155567399	175966	0	None	-501	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4588429	175966	0	None	-501	4	Mouse	6.7	pKd	=	6.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	769	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	137640475	157087	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	870	16	7	6	2.9	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4074368	157087	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	870	16	7	6	2.9	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	137649203	157508	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	894	18	8	8	3.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4079721	157508	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	894	18	8	8	3.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137653704	158633	0	None	-2	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4092424	158633	0	None	-2	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137658359	159571	0	None	-8	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4102774	159571	0	None	-8	4	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	162671821	182903	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4792291	182903	0	None	-	3	Mouse	5.7	pKd	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	132938008	159513	0	None	3	5	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4102048	159513	0	None	3	5	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	145951904	162939	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	957	14	10	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4174361	162939	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	957	14	10	10	-0.9	CCCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	145973163	163084	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1007	14	11	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4176668	163084	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	1007	14	11	11	-1.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.8b00684
	137638391	156858	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4071633	156858	0	None	-	0	Mouse	8.6	pKd	=	8.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	127047336	139798	0	None	33	4	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3798768	139798	0	None	33	4	Mouse	7.7	pKd	=	7.7	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	137644456	158313	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1010	12	9	9	1.1	C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4089149	158313	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1010	12	9	9	1.1	C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	155544852	174939	0	None	-3	5	Human	7.6	pKd	=	7.6	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4565367	174939	0	None	-3	5	Human	7.6	pKd	=	7.6	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155543031	173181	0	None	-50	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4522298	173181	0	None	-50	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155564058	175334	0	None	-794	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4574056	175334	0	None	-794	4	Mouse	7.6	pKd	=	7.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	746	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	162653604	180495	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)CN(Cc2ccccc2)C1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4753150	180495	0	None	-	0	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)CN(Cc2ccccc2)C1=O	10.1021/acsmedchemlett.9b00641
	137639815	156802	0	None	-1	4	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4071063	156802	0	None	-1	4	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137646086	157894	0	None	-	1	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	908	19	8	6	3.8	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4084136	157894	0	None	-	1	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	908	19	8	6	3.8	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137646802	157951	0	None	-	2	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4084671	157951	0	None	-	2	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	888	18	8	7	3.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	155555182	174321	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	778	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4550582	174321	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	778	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	162670795	182826	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4791112	182826	0	None	-	3	Mouse	6.6	pKd	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	137635794	156251	0	None	-	1	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	858	19	8	6	2.7	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4064881	156251	0	None	-	1	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	858	19	8	6	2.7	CC(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137642664	158080	0	None	-	3	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	772	18	9	7	-0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4086346	158080	0	None	-	3	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	772	18	9	7	-0.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	164623182	185619	0	None	-	2	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	607	11	4	4	5.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4864094	185619	0	None	-	2	Mouse	5.6	pKd	=	5.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	607	11	4	4	5.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	145959370	162007	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	959	14	11	11	-2.3	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	CHEMBL4159541	162007	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysisAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis	ChEMBL	959	14	11	11	-2.3	CCCC[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O	10.1021/acs.jmedchem.8b00684
	44310103	166647	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	77231882	166647	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	CHEMBL428134	166647	0	None	-	1	Mouse	8.5	pKd	=	8.5	Functional	Effective concentration against mouse melanocortin MC4 receptorEffective concentration against mouse melanocortin MC4 receptor	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
	162645080	179450	0	None	-	1	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	976	12	9	10	-0.9	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4740561	179450	0	None	-	1	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	976	12	9	10	-0.9	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	162649541	180055	0	None	-	0	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	963	12	9	10	-0.8	C[C@@H]1NC(=O)CN(CCN)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4747778	180055	0	None	-	0	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	963	12	9	10	-0.8	C[C@@H]1NC(=O)CN(CCN)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	155561116	174973	0	None	-7	5	Human	7.5	pKd	=	7.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4566163	174973	0	None	-7	5	Human	7.5	pKd	=	7.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	162662360	181471	0	None	-	2	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4764556	181471	0	None	-	2	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-0.8	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	155544852	174939	0	None	3	5	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4565367	174939	0	None	3	5	Mouse	7.5	pKd	=	7.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL2373991	210381	0	None	14	3	Mouse	7.5	pKd	=	7.5	Functional	Antagonistic activity against mouse Melanocortin 4 ReceptorAntagonistic activity against mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		CC[C@@H]1NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/jm049620r
	155532232	171705	0	None	-7	2	Human	6.5	pKd	=	6.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4466724	171705	0	None	-7	2	Human	6.5	pKd	=	6.5	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155562237	175709	0	None	-1548	4	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4582276	175709	0	None	-1548	4	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	692	15	8	7	0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	162654633	180644	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4754987	180644	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162672755	183090	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4794484	183090	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	164624386	186198	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	593	10	4	4	5.0	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4872932	186198	0	None	-	3	Mouse	6.5	pKd	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	593	10	4	4	5.0	CC(C)[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](Cc1ccccc1)N1C[C@@H]([C@@H](C)O)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	137634306	156322	0	None	-	2	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4065669	156322	0	None	-	2	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	164625589	185741	0	None	-	1	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	612	11	3	3	7.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	CHEMBL4866151	185741	0	None	-	1	Mouse	5.5	pKd	=	5.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay	ChEMBL	612	11	3	3	7.4	CC(C)C[C@@H]1CNC(=N)N1C[C@@H]1CCCN1[C@@H](CC1CCCCC1)N1C[C@@H](C(C)C)N(CC2CCC(C(C)(C)C)CC2)C1=N	10.1021/acs.jmedchem.0c02041
	155546131	173530	0	None	-2	5	Human	6.4	pKd	=	6.4	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4531291	173530	0	None	-2	5	Human	6.4	pKd	=	6.4	Functional	Antagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at human melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	132180599	156893	0	None	-1	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4072129	156893	0	None	-1	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137649368	157406	0	None	-6	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4078495	157406	0	None	-6	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	137653916	158580	0	None	-3	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4091894	158580	0	None	-3	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137657607	159636	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4103567	159636	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155556466	174416	0	None	-2238	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4552764	174416	0	None	-2238	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	648	17	8	6	1.2	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	155563055	175295	0	None	-75	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4573041	175295	0	None	-75	4	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	686	18	9	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	162666503	182230	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4783292	182230	0	None	-	3	Mouse	6.4	pKd	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	162662213	181496	0	None	-	3	Mouse	5.4	pKd	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4764827	181496	0	None	-	3	Mouse	5.4	pKd	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	127047624	139896	0	None	31	3	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	CHEMBL3799408	139896	0	None	31	3	Mouse	8.4	pKd	=	8.4	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
	137631920	156436	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	12	9	9	0.9	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4066929	156436	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	976	12	9	9	0.9	CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	137650523	157354	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	933	10	9	9	-0.1	C[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4077783	157354	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	933	10	9	9	-0.1	C[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL2370695	209912	0	None	-1	2	Mouse	6.3	pKd	=	6.3	Functional	Antagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysisAntagonist activity against mouse melanocortin-4 receptor (MC4R) using Schild analysis	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm010215z
	CHEMBL264190	210608	1	None	-2	8	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	137656661	159725	0	None	-	0	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1000	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4104582	159725	0	None	-	0	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1000	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL454736	213997	0	None	-	2	Mouse	8.3	pKd	=	8.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	137645343	157796	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	9	9	0.3	CCC1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4083137	157796	0	None	-	0	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	948	11	9	9	0.3	CCC1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	155561116	174973	0	None	7	5	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4566163	174973	0	None	7	5	Mouse	7.3	pKd	=	7.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	137651071	157467	0	None	-16	4	Mouse	6.3	pKd	=	6.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4079298	157467	0	None	-16	4	Mouse	6.3	pKd	=	6.3	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155566718	175916	0	None	3	2	Mouse	5.3	pKd	=	5.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4587214	175916	0	None	3	2	Mouse	5.3	pKd	=	5.3	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	155536388	172140	0	None	-	0	Human	7.3	pKd	=	7.3	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1660	36	16	19	-4.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL4473100	172140	0	None	-	0	Human	7.3	pKd	=	7.3	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1660	36	16	19	-4.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3577981	211749	1	None	-1	5	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acsmedchemlett.9b00641
	137649684	157138	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	992	13	11	11	-2.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4075125	157138	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	992	13	11	11	-2.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL3577981	211749	1	None	-1	5	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	137632217	156302	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	900	10	10	10	-2.4	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4065443	156302	0	None	-	0	Mouse	8.2	pKd	=	8.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	900	10	10	10	-2.4	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](C)NC1=O	10.1021/acs.jmedchem.7b00856
	155548853	173809	0	None	6	5	Mouse	7.2	pKd	=	7.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4538274	173809	0	None	6	5	Mouse	7.2	pKd	=	7.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	137640715	157003	0	None	-	3	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4073316	157003	0	None	-	3	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	155550083	173914	0	None	-134	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4540411	173914	0	None	-134	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	775	16	8	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.9b00053
	155558348	175036	0	None	-61	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4567480	175036	0	None	-61	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	677	19	9	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155568641	176097	0	None	-660	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4591394	176097	0	None	-660	4	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	654	14	7	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	137636060	156231	0	None	-	2	Mouse	5.2	pKd	=	5.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4064728	156231	0	None	-	2	Mouse	5.2	pKd	=	5.2	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	850	15	7	7	2.5	CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	137642489	158193	0	None	-	0	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1019	14	10	10	-0.2	CC(C)C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4087835	158193	0	None	-	0	Mouse	6.2	pKd	=	6.2	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1019	14	10	10	-0.2	CC(C)C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	127047624	139896	0	None	-	3	Human	8.1	pKd	=	8.1	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	CHEMBL3799408	139896	0	None	-	3	Human	8.1	pKd	=	8.1	Functional	Antagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced intracellular cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
	137654466	158731	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1034	16	11	11	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4093505	158731	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1034	16	11	11	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	155539948	172886	0	None	-131	4	Mouse	7.1	pKd	=	7.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4515666	172886	0	None	-131	4	Mouse	7.1	pKd	=	7.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	705	20	11	7	-0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	162647356	179680	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-1.2	CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CN)C1=O	10.1021/acsmedchemlett.9b00641
	CHEMBL4743564	179680	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assayAntagonist activity at mouse MC4R assessed as antagonist potency by alphascreen cAMP assay	ChEMBL	948	11	9	10	-1.2	CN1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N2CCC[C@@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CN)C1=O	10.1021/acsmedchemlett.9b00641
	137632948	156582	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4068643	156582	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137651782	157493	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4079580	157493	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	137646614	157538	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4080138	157538	0	None	-	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	822	18	9	7	0.9	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
	155547310	173611	0	None	-	3	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	750	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	CHEMBL4533593	173611	0	None	-	3	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	750	17	7	7	0.5	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O	10.1021/acs.jmedchem.9b00053
	155565321	175576	0	None	-100	4	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	CHEMBL4579448	175576	0	None	-100	4	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene assessed as inhibition of NDP-MSH-induced cAMP accumulation up to 10 uM after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL	718	13	5	6	0.7	CC(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acs.jmedchem.9b00053
	137631703	156403	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	12	10	10	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4066514	156403	0	None	-	0	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	962	12	10	10	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	155532232	171705	0	None	7	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL4466724	171705	0	None	7	2	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
	CHEMBL103817	208459	0	None	2	4	Mouse	8.1	pKd	=	8.1	Functional	Antagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assayAntagonist activity against mouse MC4R expressed in HEK293 cells assessed as NDP-MSH-stimulated cAMP accumulation incubated for 2 hrs by alphascreen assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
	137640194	156959	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1043	14	11	11	-1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	CHEMBL4072797	156959	0	None	-	1	Mouse	6.1	pKd	=	6.1	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assayAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation after 2 hrs by AlphaScreen assay	ChEMBL	1043	14	11	11	-1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.7b00856
	127035019	136436	0	None	-	1	Mouse	9.3	pKi	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	136436	0	None	-	1	Mouse	9.3	pKi	=	9.3	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	137655051	158966	0	None	-	0	Human	9.1	pKi	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4096081	158966	0	None	-	0	Human	9.1	pKi	=	9.1	Functional	Antagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 minsAntagonist activity at human MC4R expressed in CHO cells assessed as inhibition of aplha MSH-induced cAMP activation after 45 mins	ChEMBL	791	15	9	6	1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc(I)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
	127035019	136436	0	None	-	1	Mouse	9.1	pKi	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	CHEMBL3735607	136436	0	None	-	1	Mouse	9.1	pKi	=	9.1	Functional	Antagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysisAntagonist activity at mouse MC4 receptor expressed in HEK293 cells assessed as NDP-MSH induced response by cAMP alpha screen based schild analysis	ChEMBL	1074	17	14	11	0.1	CCCCC(NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2015.10.095
	162664463	182190	0	None	-	3	Mouse	5.0	pKi	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4782762	182190	0	None	-	3	Mouse	5.0	pKi	=	5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162673830	183159	0	None	-	3	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4795352	183159	0	None	-	3	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	137642804	158371	0	None	-	1	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4089759	158371	0	None	-	1	Mouse	6.9	pKi	=	6.9	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	832	18	8	6	2.2	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
	132180598	157849	0	None	-25	4	Mouse	7.8	pKi	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	CHEMBL4083717	157849	0	None	-25	4	Mouse	7.8	pKi	=	7.8	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as inhibition of NDP-MSH induced-cAMP accumulation after 2 hrs by alpha screen assay	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
	2804382	100345	3	None	-	0	Mouse	4.8	pKi	=	4.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	318	4	1	3	4.0	Fc1cccc(F)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL289532	100345	3	None	-	0	Mouse	4.8	pKi	=	4.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	318	4	1	3	4.0	Fc1cccc(F)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	162649653	180100	0	None	-	3	Mouse	6.8	pKi	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4748317	180100	0	None	-	3	Mouse	6.8	pKi	=	6.8	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	753	18	10	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	9842665	156806	12	None	-	1	Mouse	6.8	pKi	=	6.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm034244g
	CHEMBL40711	156806	12	None	-	1	Mouse	6.8	pKi	=	6.8	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm034244g
	CHEMBL454736	213997	0	None	-	2	Mouse	7.7	pKi	=	7.7	Functional	Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assayAntagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm800291b
	162671821	182903	0	None	-	3	Mouse	5.7	pKi	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4792291	182903	0	None	-	3	Mouse	5.7	pKi	=	5.7	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	725	17	8	7	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	9864301	155177	0	None	-	0	Mouse	6.7	pKi	=	6.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	372	5	1	3	4.0	COc1ccc(Br)cc1CCc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL40233	155177	0	None	-	0	Mouse	6.7	pKi	=	6.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	372	5	1	3	4.0	COc1ccc(Br)cc1CCc1ccccc1C1=NCCCN1	10.1021/jm034244g
	2806083	100159	3	None	-	0	Mouse	5.7	pKi	=	5.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	356	4	1	4	5.1	Clc1cc(CSc2ccccc2C2=NCCCN2)c(Cl)s1	10.1021/jm034244g
	CHEMBL287895	100159	3	None	-	0	Mouse	5.7	pKi	=	5.7	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	356	4	1	4	5.1	Clc1cc(CSc2ccccc2C2=NCCCN2)c(Cl)s1	10.1021/jm034244g
	162670795	182826	0	None	-	3	Mouse	6.6	pKi	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4791112	182826	0	None	-	3	Mouse	6.6	pKi	=	6.6	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	605683	158030	3	None	-	0	Mouse	5.6	pKi	=	5.6	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	334	4	1	3	4.5	Fc1cccc(Cl)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL40857	158030	3	None	-	0	Mouse	5.6	pKi	=	5.6	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	334	4	1	3	4.5	Fc1cccc(Cl)c1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	162654633	180644	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4754987	180644	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162672755	183090	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4794484	183090	0	None	-	3	Mouse	6.5	pKi	=	6.5	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	734	16	8	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	11245316	168510	0	None	-	0	Mouse	7.4	pKi	=	7.4	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	358	5	1	3	3.6	COc1ccc(Br)cc1CCc1ccccc1C1=NCCN1	10.1021/jm034244g
	CHEMBL435368	168510	0	None	-	0	Mouse	7.4	pKi	=	7.4	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	358	5	1	3	3.6	COc1ccc(Br)cc1CCc1ccccc1C1=NCCN1	10.1021/jm034244g
	162662213	181496	0	None	-	3	Mouse	5.4	pKi	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	CHEMBL4764827	181496	0	None	-	3	Mouse	5.4	pKi	=	5.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	706	15	6	7	1.0	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/acsmedchemlett.0c00561
	162666503	182230	0	None	-	3	Mouse	6.4	pKi	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	CHEMBL4783292	182230	0	None	-	3	Mouse	6.4	pKi	=	6.4	Functional	Antagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysisAntagonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as inhibition of NDP-MSH-induced cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay based Schild analysis	ChEMBL	696	15	7	6	1.7	CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O)C(C)C	10.1021/acsmedchemlett.0c00561
	10293816	162176	0	None	-	0	Mouse	7.2	pKi	=	7.2	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	390	5	1	4	4.5	COc1ccc(Br)cc1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	CHEMBL416244	162176	0	None	-	0	Mouse	7.2	pKi	=	7.2	Functional	Antagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assayAntagonistic activity against mice melanocortin 4 receptor using [125I][NDP]-R-MSH as radioligand in a membrane filtration assay	ChEMBL	390	5	1	4	4.5	COc1ccc(Br)cc1CSc1ccccc1C1=NCCCN1	10.1021/jm034244g
	129627786	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	1330	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16129617	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16129674	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16133751	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16133802	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	16162116	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	3767	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	4516	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	60210072	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	6965	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	CHEMBL2103784	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	DB01284	280	32	None	-	1	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		None	None
	131839615	212636	26	None	-1	7	Mouse	8.0	pEC50	=	8	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
	16133835	212636	26	None	-1	7	Mouse	8.0	pEC50	=	8	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
	CHEMBL407070	212636	26	None	-1	7	Mouse	8.0	pEC50	=	8	Functional	Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrsAgonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
	1339	2465	0	None	-	1	Human	10.0	pIC50	=	10	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11606131
	1338	3807	43	None	-2	8	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	12361385
	9938402	3807	43	None	-2	8	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	12361385
	CHEMBL339053	3807	43	None	-2	8	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	12361385
	1341	3076	0	None	-251	3	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	12431055
	1337	3424	6	None	3	5	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	15982875
	6918851	3424	6	None	3	5	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	15982875
	CHEMBL364346	3424	6	None	3	5	Human	8.1	pIC50	None	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	15982875
	1335	315	0	None	39	3	Human	9.3	pIC50	None	9.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9299416

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Similar- ity	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
		1046	202652	116	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	123	1	1	3	-0.4	NC(=O)c1cnccn1	10.1038/s41467-023-40064-9
		CHEMBL614	202652	116	None	-	0	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	123	1	1	3	-0.4	NC(=O)c1cnccn1	10.1038/s41467-023-40064-9
		68617	205527	62	None	-	26	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
		CHEMBL1709	205527	62	None	-	26	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
		CHEMBL809	205527	62	None	-	26	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	305	2	1	1	5.2	CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21	10.1038/s41467-023-40064-9
		1016	3747	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		2561	3747	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		2733526	3747	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		5384	3747	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL83	3747	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		DB00675	3747	78	None	-70	35	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
		4212	198679	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
		CHEMBL1417019	198679	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
		CHEMBL58	198679	82	None	-	4	Human	4.9	pAC50	=	4.9	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
		2351	4300	49	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
		CHEMBL1008	4300	49	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
		CHEMBL1257078	4300	49	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	366	10	0	3	4.8	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	10.1038/s41467-023-40064-9
		1155	1629	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		3343	1629	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		557	1629	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		CHEMBL32800	1629	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		DB01288	1629	53	None	-	5	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	303	6	5	5	2.1	CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O	10.1038/s41467-023-40064-9
		2162	41514	100	None	-	6	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	408	8	2	7	2.3	CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl	10.1038/s41467-023-40064-9
		CHEMBL1491	41514	100	None	-	6	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	408	8	2	7	2.3	CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl	10.1038/s41467-023-40064-9
		1212	1662	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		204	1662	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		3372	1662	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		CHEMBL726	1662	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		DB00623	1662	50	None	-	65	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		1222	1664	49	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		3396	1664	49	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		85	1664	49	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL46516	1664	49	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		DB04842	1664	49	None	-	33	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	475	7	1	3	5.3	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1	10.1038/s41467-023-40064-9
		2726	919	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		621	919	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		83	919	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		CHEMBL71	919	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		DB00477	919	68	None	-154	72	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		16362	3125	71	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		2172	3125	71	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		90	3125	71	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		CHEMBL1423	3125	71	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		DB01100	3125	71	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
		25077405	2715	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		3902	2715	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		CHEMBL1201309	2715	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		DB00666	2715	0	None	-	1	Human	5.8	pAC50	=	5.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
		180	401	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		200	401	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		2160	401	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		CHEMBL629	401	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		DB00321	401	56	None	-	40	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		5328940	100216	107	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	529	9	1	8	5.2	COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl	10.1038/s41467-023-40064-9
		CHEMBL288441	100216	107	None	-	0	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	529	9	1	8	5.2	COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl	10.1038/s41467-023-40064-9
		202	1508	77	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		60835	1508	77	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		972	1508	77	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		CHEMBL1175	1508	77	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		DB00476	1508	77	None	-	30	Human	4.8	pAC50	=	4.8	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	297	6	1	3	4.6	CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2	10.1038/s41467-023-40064-9
		11626560	200937	94	None	-	0	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	449	5	2	6	5.0	C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl	10.1038/s41467-023-40064-9
		CHEMBL601719	200937	94	None	-	0	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	449	5	2	6	5.0	C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl	10.1038/s41467-023-40064-9
		1353	1911	93	None	-	83	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		3559	1911	93	None	-	83	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		86	1911	93	None	-	83	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		CHEMBL54	1911	93	None	-	83	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		DB00502	1911	93	None	-	83	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
		1427	2013	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		357	2013	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		3696	2013	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		CHEMBL11	2013	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		DB00458	2013	54	None	-	27	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
		176	398	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		2157	398	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		2566	398	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		CHEMBL633	398	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		DB01118	398	66	None	-6	31	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
		4046	2483	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		4252	2483	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		CHEMBL416956	2483	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		DB00358	2483	33	None	-	2	Human	4.7	pAC50	=	4.7	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		3676	205270	101	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	234	5	1	2	2.6	CCN(CC)CC(=O)Nc1c(C)cccc1C	10.1038/s41467-023-40064-9
		CHEMBL79	205270	101	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	234	5	1	2	2.6	CCN(CC)CC(=O)Nc1c(C)cccc1C	10.1038/s41467-023-40064-9
		1056	3371	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		2405	3371	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		77999	3371	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		CHEMBL121	3371	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		DB00412	3371	116	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	357	7	1	6	2.5	O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C	10.1038/s41467-023-40064-9
		4046	2483	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		4252	2483	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		CHEMBL416956	2483	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		DB00358	2483	33	None	-	2	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	378	2	2	3	4.4	OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1	10.1038/s41467-023-40064-9
		5090	15561	106	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	3	0	4	2.6	CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1	10.1038/s41467-023-40064-9
		CHEMBL122	15561	106	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	3	0	4	2.6	CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1	10.1038/s41467-023-40064-9
		4236	28096	66	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	273	5	1	2	2.0	NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL1373	28096	66	None	-	1	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	273	5	1	2	2.0	NC(=O)C[S+]([O-])C(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		2286	3183	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		4927	3183	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		7282	3183	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		CHEMBL643	3183	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		DB01069	3183	51	None	-	30	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
		3899	207774	119	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	270	2	1	3	3.3	Cc1oncc1C(=O)Nc1ccc(C(F)(F)F)cc1	10.1038/s41467-023-40064-9
		CHEMBL960	207774	119	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	270	2	1	3	3.3	Cc1oncc1C(=O)Nc1ccc(C(F)(F)F)cc1	10.1038/s41467-023-40064-9
		16220172	73043	95	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	392	2	3	3	5.1	CC(C)(C)c1cc(C(C)(C)C)c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O	10.1038/s41467-023-40064-9
		CHEMBL2010601	73043	95	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	392	2	3	3	5.1	CC(C)(C)c1cc(C(C)(C)C)c(NC(=O)c2c[nH]c3ccccc3c2=O)cc1O	10.1038/s41467-023-40064-9
		2713	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		5353524	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		5360566	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		88536661	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		9552079	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		CHEMBL1330113	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		CHEMBL790	205271	82	None	-	0	Human	6.6	pAC50	=	6.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	504	9	10	4	4.2	N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1	10.1038/s41467-023-40064-9
		6436173	55116	45	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	785	2	5	13	6.2	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
		CHEMBL1617	55116	45	None	-	0	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	785	2	5	13	6.2	CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C	10.1038/s41467-023-40064-9
		104850	3330	96	None	-	5	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		4150	3330	96	None	-	5	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		743	3330	96	None	-	5	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		CHEMBL111	3330	96	None	-	5	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		DB06155	3330	96	None	-	5	Human	4.6	pAC50	=	4.6	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
		124087	1389	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		7157	1389	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		814	1389	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		CHEMBL1172	1389	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		DB00967	1389	114	None	-	15	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
		2200	20203	61	None	-	2	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
		CHEMBL1256819	20203	61	None	-	2	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
		CHEMBL1305	20203	61	None	-	2	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	265	5	1	3	2.7	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	10.1038/s41467-023-40064-9
		26987	949	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		6063	949	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		671	949	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		CHEMBL1626	949	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		DB00283	949	33	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	10.1038/s41467-023-40064-9
		2585	803	103	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		522	803	103	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		551	803	103	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		CHEMBL723	803	103	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		DB01136	803	103	None	-	21	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
		2812	4779	101	None	-	34	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
		CHEMBL104	4779	101	None	-	34	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
		2398	954	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		2801	954	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		701	954	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		CHEMBL415	954	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		DB01242	954	62	None	-	29	Human	4.5	pAC50	=	4.5	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
		54675785	94213	42	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	442	2	6	9	-0.4	C=C1c2cccc(O)c2C(=O)C2=C(O)[C@]3(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]3[C@@H](O)[C@H]12	10.1038/s41467-023-40064-9
		CHEMBL249837	94213	42	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	442	2	6	9	-0.4	C=C1c2cccc(O)c2C(=O)C2=C(O)[C@]3(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]3[C@@H](O)[C@H]12	10.1038/s41467-023-40064-9
		10096344	89594	85	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	472	4	1	10	1.1	CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C	10.1038/s41467-023-40064-9
		CHEMBL237500	89594	85	None	-	0	Human	4.4	pAC50	=	4.4	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	472	4	1	10	1.1	CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C	10.1038/s41467-023-40064-9
		135409453	3773	41	None	-	2	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	301	7	3	3	2.6	CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N	10.1038/s41467-023-40064-9
		226	3773	41	None	-	2	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	301	7	3	3	2.6	CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N	10.1038/s41467-023-40064-9
		CHEMBL76370	3773	41	None	-	2	Human	5.3	pAC50	=	5.3	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	301	7	3	3	2.6	CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N	10.1038/s41467-023-40064-9
		9801	91585	35	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	329	8	1	1	5.4	CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		CHEMBL24072	91585	35	None	-	0	Human	5.2	pAC50	=	5.2	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	329	8	1	1	5.4	CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1	10.1038/s41467-023-40064-9
		2600	3779	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		2608	3779	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		5405	3779	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		CHEMBL17157	3779	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		DB00342	3779	74	None	-	13	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
		8550	14424	57	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	578	7	1	9	4.2	COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC	10.1038/s41467-023-40064-9
		CHEMBL1200515	14424	57	None	-	0	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	578	7	1	9	4.2	COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC	10.1038/s41467-023-40064-9
		2274	3173	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		4917	3173	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		7279	3173	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		CHEMBL728	3173	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		DB00433	3173	58	None	-	31	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	373	4	0	4	4.6	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
		214	3860	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		2740	3860	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		5566	3860	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		66064	3860	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		CHEMBL422	3860	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		DB00831	3860	58	None	-	30	Human	5.1	pAC50	=	5.1	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
		100	3805	58	None	-	55	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		2637	3805	58	None	-	55	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		5452	3805	58	None	-	55	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		CHEMBL479	3805	58	None	-	55	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		DB00679	3805	58	None	-	55	Human	5.0	pAC50	=	5.0	Binding	Binding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular componentsBinding affinity towards human MC4R in an in vitro assay with cellular components measured by scintillation proximity assay in vitro assay with cellular components	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	10.1038/s41467-023-40064-9
		1324	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		16154396	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		16197727	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		44285019	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		57514683	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		91898441	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		CHEMBL441738	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		DB04931	302	25	None	-3	4	Human	10.8	pEC50	=	10.8	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		1323	2688	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/ml500340z
		92432	2688	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/ml500340z
		CHEMBL430239	2688	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		None	10.1021/ml500340z
		1323	2688	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		92432	2688	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		CHEMBL430239	2688	55	None	-	3	Mouse	10.3	pEC50	=	10.3	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		1323	2688	55	None	-10	3	Human	10.2	pEC50	=	10.2	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		92432	2688	55	None	-10	3	Human	10.2	pEC50	=	10.2	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		CHEMBL430239	2688	55	None	-10	3	Human	10.2	pEC50	=	10.2	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm0303103
		1323	2688	55	None	-	3	Mouse	10.1	pEC50	=	10.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		92432	2688	55	None	-	3	Mouse	10.1	pEC50	=	10.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		CHEMBL430239	2688	55	None	-	3	Mouse	10.1	pEC50	=	10.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		44327392	141863	0	None	-	0	Mouse	10.1	pEC50	=	10.1	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	1025	21	12	12	-0.6	CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O	10.1021/jm0104872
		CHEMBL386583	141863	0	None	-	0	Mouse	10.1	pEC50	=	10.1	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	1025	21	12	12	-0.6	CCCC[C@H](NC(C)=O)C(=O)N1C(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]1CC(=O)O	10.1021/jm0104872
		CHEMBL2369959	209740	0	None	-	0	Mouse	9.9	pEC50	=	9.9	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		1324	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		16154396	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		16197727	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		44285019	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		57514683	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		91898441	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		CHEMBL441738	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		DB04931	302	25	None	-	4	Mouse	9.8	pEC50	=	9.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm049010r
		CHEMBL217305	209373	0	None	-	0	Human	9.8	pEC50	=	9.8	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1016/s0960-894x(03)00412-8
		CHEMBL415165	213176	0	None	-3	5	Human	9.7	pEC50	=	9.7	Binding	Effective concentration against human melanocortin-4 receptor Effective concentration against human melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm0501432
		1324	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		16154396	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		16197727	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		44285019	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		57514683	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		91898441	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		CHEMBL441738	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		DB04931	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm020296e
		16132144	209279	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		16133793	209279	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		44273719	209279	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		CHEMBL214332	209279	36	None	-30	4	Human	9.7	pEC50	=	9.7	Binding	Effective concentration required for the biological activity against human Melanocortin 4 receptorEffective concentration required for the biological activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0303103
		1324	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		16154396	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		16197727	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		44285019	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		57514683	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		91898441	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		CHEMBL441738	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		DB04931	302	25	None	-	4	Mouse	9.7	pEC50	=	9.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		None	10.1021/jm0104872
		CHEMBL2369963	209744	0	None	-	0	Mouse	9.6	pEC50	=	9.6	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369967	209748	0	None	-	0	Mouse	9.4	pEC50	=	9.4	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL365913	212043	0	None	-	0	Human	9.3	pEC50	=	9.3	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2369975	209756	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369982	209763	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369971	209752	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369960	209741	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369983	209764	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369964	209745	0	None	-	0	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		118720368	115878	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354737	115878	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720368	115878	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354737	115878	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3128	92	35	40	-5.9	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720369	115879	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354738	115879	0	None	-	0	Human	8.9	pEC50	=	8.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354729	211551	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354736	211555	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		155527254	171250	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
		CHEMBL4460053	171250	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1038	17	14	11	-0.6	CCCCC(NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3354729	211551	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354736	211555	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		44322795	206926	0	None	13	3	Human	8.8	pEC50	=	8.8	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL91041	206926	0	None	13	3	Human	8.8	pEC50	=	8.8	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		118720370	115880	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354739	115880	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720370	115880	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354739	115880	0	None	-	0	Human	8.8	pEC50	=	8.8	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2665	83	32	34	-3.2	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720363	115876	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354732	115876	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720363	115876	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354732	115876	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2406	52	29	27	-0.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720364	115877	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354733	115877	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720369	115879	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354738	115879	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2347	65	30	28	-2.3	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720364	115877	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354733	115877	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2724	70	31	33	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		16132144	209279	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		16133793	209279	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		44273719	209279	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		CHEMBL214332	209279	36	None	-	4	Mouse	8.7	pEC50	=	8.7	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049010r
		CHEMBL3354730	211552	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354735	211554	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL188738	209059	0	None	-	0	Human	7.0	pEC50	=	7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL154251	208801	0	None	-	0	Mouse	6.0	pEC50	=	6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/jm020296e
		CHEMBL330233	211331	0	None	-	0	Mouse	6.0	pEC50	=	6	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL3354743	211559	0	None	-	0	Human	8.0	pEC50	=	8.0	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		CHEMBL2369961	209742	0	None	-	0	Mouse	6.9	pEC50	=	6.9	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCc3ccccc3C2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL152555	208795	0	None	-	0	Mouse	4.9	pEC50	=	4.9	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C(N)=O)C(c1ccccc1)c1ccccc1	10.1021/jm020296e
		CHEMBL275303	210821	0	None	-	0	Mouse	4.9	pEC50	=	4.9	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		101728563	161760	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44308542	161760	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932720	161760	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL413936	161760	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1383	39	18	14	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		155551846	175134	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
		CHEMBL4569789	175134	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1589	48	22	20	-3.2	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.8b00238
		44322868	106008	0	None	-37	3	Human	5.9	pEC50	=	5.9	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313279	106008	0	None	-37	3	Human	5.9	pEC50	=	5.9	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44308622	168875	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2236	84	25	27	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932727	168875	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2236	84	25	27	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL438237	168875	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2236	84	25	27	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		101728568	96762	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		44387459	96762	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		91932729	96762	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL264577	96762	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1550	40	19	15	1.8	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)N[C@@H](Cc3c[nH]cn3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL190953	209077	0	None	-	0	Human	5.9	pEC50	=	5.9	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL2371827	210132	0	None	-	0	Human	5.9	pEC50	=	5.9	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1021/jm0490033
		CHEMBL317968	211207	0	None	-	0	Mouse	6.9	pEC50	=	6.9	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccncc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL3354724	211550	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354724	211550	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		127047475	139749	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		132991507	139749	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3798421	139749	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL268082	210739	0	None	-	0	Human	7.9	pEC50	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		127047913	139924	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3799563	139924	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL151906	208794	0	None	-	0	Mouse	6.8	pEC50	=	6.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(N)=O	10.1021/jm020296e
		101728566	161749	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44387460	161749	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932726	161749	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL413842	161749	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1511	44	20	16	-2.5	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL2369968	209749	0	None	-	0	Mouse	4.8	pEC50	=	4.8	Binding	Effective concentration for mouse Melanocortin-4 receptor at 100 uMEffective concentration for mouse Melanocortin-4 receptor at 100 uM	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC1=O	10.1021/jm049010r
		44308621	168913	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2250	68	29	24	-2.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932722	168913	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2250	68	29	24	-2.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL438577	168913	0	None	-	0	Human	7.8	pEC50	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2250	68	29	24	-2.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL357558	211743	0	None	-	0	Mouse	7.8	pEC50	=	7.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/jm020296e
		CHEMBL348901	211716	0	None	-	0	Mouse	5.8	pEC50	=	5.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/jm020296e
		CHEMBL3799094	212268	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL320157	211226	0	None	-	0	Mouse	5.8	pEC50	=	5.8	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL329490	211317	0	None	-	0	Mouse	5.8	pEC50	=	5.8	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL191063	209079	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL191120	209080	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		127047209	139812	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3798845	139812	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1610	36	16	19	-5.7	CC(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCNC(=N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(=O)N1CCCC1C(=O)NCC(N)=O	10.1021/acs.jmedchem.8b00238
		101728572	161852	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		44387457	161852	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		91932734	161852	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL414723	161852	0	None	-	0	Human	6.8	pEC50	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1669	42	20	16	3.1	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)Nc2ccc(C(=O)Nc3ccc(C(=O)N[C@@H](Cc4c[nH]cn4)C(=O)N[C@H](Cc4ccccc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc4c[nH]c5ccccc45)C(N)=O)cc3)cc2)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL2369972	209753	0	None	-	0	Mouse	4.8	pEC50	=	4.8	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44369234	45246	0	None	-	0	Mouse	7.8	pEC50	=	7.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL	685	18	9	7	-0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm020296e
		CHEMBL152612	45246	0	None	-	0	Mouse	7.8	pEC50	=	7.8	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL	685	18	9	7	-0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm020296e
		CHEMBL264190	210608	1	None	39	2	Mouse	7.8	pEC50	=	7.8	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL3354742	211558	0	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		CHEMBL186970	209054	0	None	-	0	Human	7.7	pEC50	=	7.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		127048118	173007	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL4518266	173007	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	2236	54	25	25	-5.6	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL189991	209061	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL190834	209069	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371823	210131	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1	10.1021/jm0490033
		CHEMBL2371828	210133	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)C(C)=O	10.1021/jm0490033
		CHEMBL2371832	210135	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL3354730	211552	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354735	211554	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720362	115875	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354731	115875	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720362	115875	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354731	115875	0	None	-	0	Human	8.7	pEC50	=	8.7	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	3187	79	34	39	-3.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](CCCC)C(=O)N[C@H]2CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3cnc[nH]3)NC2=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL373344	212175	0	None	-	0	Human	8.6	pEC50	=	8.6	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		44269217	30260	0	None	-	0	Human	8.5	pEC50	=	8.5	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	649	14	3	6	4.4	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1	10.1021/jm025600i
		CHEMBL13910	30260	0	None	-	0	Human	8.5	pEC50	=	8.5	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	649	14	3	6	4.4	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)c2ccccc2)CC1	10.1021/jm025600i
		CHEMBL2370154	209801	0	None	1	3	Human	8.5	pEC50	=	8.5	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm020021z
		10101361	155703	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL405174	155703	0	None	-	1	Mouse	7.7	pEC50	=	7.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	717	16	8	6	2.4	CC(=O)Nc1cc2ccccc2cc1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL431092	213622	0	None	-	0	Mouse	6.7	pEC50	=	6.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL329847	211321	0	None	-	0	Mouse	5.7	pEC50	=	5.7	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		44323212	168719	0	None	-1	2	Human	7.7	pEC50	=	7.7	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		CHEMBL436903	168719	0	None	-1	2	Human	7.7	pEC50	=	7.7	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		44269189	98338	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	587	13	3	6	3.1	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1	10.1021/jm025600i
		CHEMBL275067	98338	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	587	13	3	6	3.1	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(C)=O)CC1	10.1021/jm025600i
		46877881	201818	0	None	2	3	Human	5.6	pEC50	=	5.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL606990	201818	0	None	2	3	Human	5.6	pEC50	=	5.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		101728569	159731	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44308747	159731	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932733	159731	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL410471	159731	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1639	49	22	18	-3.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		101728567	161787	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		44387462	161787	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932731	161787	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL414101	161787	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1542	48	19	17	-1.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL3354741	211557	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		44308558	168874	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2506	78	33	28	-4.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932730	168874	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2506	78	33	28	-4.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL438228	168874	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	2506	78	33	28	-4.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCCN)C(=O)CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		118720357	115873	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354726	115873	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL264190	210608	1	None	39	2	Mouse	6.6	pEC50	=	6.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm020296e
		118720357	115873	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354726	115873	0	None	-	0	Human	7.6	pEC50	=	7.6	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1392	35	16	17	-0.8	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL190080	209062	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371835	210137	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL154153	208800	0	None	-	0	Mouse	6.6	pEC50	=	6.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccc2ccccc12)C(N)=O	10.1021/jm020296e
		CHEMBL2369966	209747	0	None	-	0	Mouse	6.6	pEC50	=	6.6	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2Cc3ccccc3CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44323234	168056	0	None	-7	3	Human	6.6	pEC50	=	6.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL432377	168056	0	None	-7	3	Human	6.6	pEC50	=	6.6	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		9915813	38489	15	None	-	0	Human	5.6	pEC50	=	5.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	559	12	2	7	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1	10.1021/jm025600i
		CHEMBL14642	38489	15	None	-	0	Human	5.6	pEC50	=	5.6	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	559	12	2	7	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](N)Cc2cncn2C)CC1	10.1021/jm025600i
		CHEMBL407694	212678	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL347364	211713	0	None	-	0	Mouse	5.6	pEC50	=	5.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/jm020296e
		CHEMBL350012	211722	0	None	-	0	Mouse	4.6	pEC50	=	4.6	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]cn1)C(N)=O	10.1021/jm020296e
		127047853	139993	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3799955	139993	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL264190	210608	1	None	-	2	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL94369	215908	0	None	-	0	Mouse	5.5	pEC50	=	5.5	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL96871	215921	0	None	-	0	Mouse	5.5	pEC50	=	5.5	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N1Cc2ccccc2C[C@H]1C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		118720356	115872	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354725	115872	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720356	115872	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354725	115872	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	2172	62	21	29	-4.4	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354722	211548	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		10260053	168203	0	None	-4	3	Human	5.5	pEC50	=	5.5	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		CHEMBL433413	168203	0	None	-4	3	Human	5.5	pEC50	=	5.5	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		CHEMBL433522	213641	0	None	-	0	Mouse	4.5	pEC50	=	4.5	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccncc1)C(N)=O	10.1021/jm020296e
		CHEMBL365262	212037	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL372237	212172	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371833	210136	0	None	-	0	Human	5.5	pEC50	=	5.5	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL2369969	209750	0	None	-	0	Mouse	7.5	pEC50	=	7.5	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44308639	169038	0	None	-	0	Human	7.5	pEC50	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1948	68	23	22	-0.0	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932721	169038	0	None	-	0	Human	7.5	pEC50	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1948	68	23	22	-0.0	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL439484	169038	0	None	-	0	Human	7.5	pEC50	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1948	68	23	22	-0.0	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL2371147	210017	0	None	-	0	Mouse	5.5	pEC50	=	5.5	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1	10.1021/jm020296e
		101728564	155165	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		44308543	155165	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		91932719	155165	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL402257	155165	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1431	38	18	14	0.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccc(C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)cc1	10.1016/j.bmcl.2003.09.079
		CHEMBL2096745	209207	0	None	-	0	Mouse	4.4	pEC50	=	4.4	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@@H]1C(N)=O	10.1021/jm020296e
		CHEMBL365794	212041	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190427	209065	0	None	-	0	Human	5.4	pEC50	=	5.4	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL3354722	211548	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		6918707	104192	1	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	104192	1	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL3354734	211553	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354734	211553	0	None	-	0	Human	8.4	pEC50	=	8.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		44269245	167221	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	602	7	2	6	2.8	COc1ccc(C[C@@H](NC(=O)[C@H]2Cc3ccccc3CN2)C(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1	10.1021/jm025600i
		CHEMBL429212	167221	0	None	-	0	Human	7.4	pEC50	=	7.4	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	602	7	2	6	2.8	COc1ccc(C[C@@H](NC(=O)[C@H]2Cc3ccccc3CN2)C(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1	10.1021/jm025600i
		118720358	115874	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354727	115874	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		118720358	115874	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354727	115874	0	None	-	0	Human	6.4	pEC50	=	6.4	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL	1710	53	18	23	-1.7	CCCC[C@H](NC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL2369965	209746	0	None	-	0	Mouse	7.4	pEC50	=	7.4	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2369976	209757	0	None	-	0	Mouse	5.4	pEC50	=	5.4	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2371150	210018	0	None	-	0	Mouse	4.4	pEC50	=	4.4	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(N)=O	10.1021/jm020296e
		71152492	160064	2	None	-	0	Human	5.4	pEC50	=	5.4	Binding	Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.	ChEMBL	530	12	2	5	3.9	COc1ccc(C[C@@H](NC(=O)CCc2nc[nH]c2C)C(=O)N2CC(OCC3CC3)(c3ccccc3C)C2)cc1	nan
		CHEMBL4108378	160064	2	None	-	0	Human	5.4	pEC50	=	5.4	Binding	Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.Transactivation Assay: The products are dissolved at 10 mM in DMSO. They are tested as a response dose at 0.1% of DMSO final. The range comprising 10 points and a zero starts at 10 μM with four-fold dilutions. To test agonists, the products are tested alone. To determine the antagonist behaviour, the products of interest are tested in the presence of 1 nM NDP-MSH (reference agonist). The cells are inoculated at a rate of 5000 cells per well (384-well plate) in serum-free DMEM medium and incubated overnight at 37° C. and 5% CO2. The products and the reference ligand (NDP-MSH) are added the following day and the plates are reincubated for 6 hours at 37° C. and 5% CO2. After adding the lysis buffer containing luciferin, the plates are read in a Top-Count machine.	ChEMBL	530	12	2	5	3.9	COc1ccc(C[C@@H](NC(=O)CCc2nc[nH]c2C)C(=O)N2CC(OCC3CC3)(c3ccccc3C)C2)cc1	nan
		CHEMBL347216	211712	0	None	-	0	Mouse	7.3	pEC50	=	7.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/jm020296e
		16132144	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		16133793	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		44273719	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		CHEMBL214332	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm020296e
		16132144	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		16133793	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		44273719	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		CHEMBL214332	209279	36	None	-	4	Mouse	8.3	pEC50	=	8.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm0104872
		CHEMBL264190	210608	1	None	39	2	Mouse	8.3	pEC50	=	8.3	Binding	Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml500340z
		44322869	106160	0	None	-6	3	Human	7.3	pEC50	=	7.3	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313690	106160	0	None	-6	3	Human	7.3	pEC50	=	7.3	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44360829	165748	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	550	8	3	6	1.3	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		CHEMBL424661	165748	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Evaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulationEvaluated for Functional Activity at Melanocortin-4 receptor as effective concentration at 50% maximum CMP accumulation	ChEMBL	550	8	3	6	1.3	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		CHEMBL275999	210826	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL371610	212170	0	None	-	0	Human	5.3	pEC50	=	5.3	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL94391	215909	0	None	-	0	Mouse	6.3	pEC50	=	6.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL432201	213633	0	None	-	0	Mouse	6.3	pEC50	=	6.3	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL346925	211711	0	None	-	0	Mouse	5.3	pEC50	=	5.3	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O	10.1021/jm020296e
		127046235	139638	0	None	-	0	Human	7.3	pEC50	=	7.3	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
		CHEMBL3797690	139638	0	None	-	0	Human	7.3	pEC50	=	7.3	Binding	Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assayAgonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.8b00238
		44308380	96670	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1767	54	24	20	-5.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932732	96670	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1767	54	24	20	-5.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL263874	96670	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1767	54	24	20	-5.3	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL2304247	209484	0	None	-	0	Mouse	8.2	pEC50	=	8.2	Binding	Displacement of MT2 from mouse MC4R expressed in HEK293 cellsDisplacement of MT2 from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
		CHEMBL3350327	211470	0	None	-	0	Mouse	8.2	pEC50	=	8.2	Binding	Displacement of MT2 from mouse MC4R expressed in HEK293 cellsDisplacement of MT2 from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)O	10.1021/jm0492756
		CHEMBL432027	213631	0	None	-	0	Mouse	5.2	pEC50	=	5.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL188459	209057	0	None	-	0	Human	7.2	pEC50	=	7.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		11038873	171880	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	545	12	3	6	2.9	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL446941	171880	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	545	12	3	6	2.9	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](N)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL190203	209064	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL370321	212167	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL364711	212032	0	None	-	0	Human	5.2	pEC50	=	5.2	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		44387458	168932	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1600	52	19	18	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		91932725	168932	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1600	52	19	18	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		CHEMBL438749	168932	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1600	52	19	18	-1.2	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCNC(=O)CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2003.09.079
		6918707	104192	1	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	104192	1	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)Intracellular levels of cAMP in HEK 293 cells expressing human melanocortin 4 receptor (hMC4R)	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		44308379	160214	0	None	-	0	Human	8.2	pEC50	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1859	60	24	20	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932724	160214	0	None	-	0	Human	8.2	pEC50	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1859	60	24	20	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL410966	160214	0	None	-	0	Human	8.2	pEC50	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1859	60	24	20	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCC(=O)NCC(=O)NCCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		44323233	106716	0	None	4	2	Human	7.2	pEC50	=	7.2	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL314401	106716	0	None	4	2	Human	7.2	pEC50	=	7.2	Binding	Inhibition of binding to human Melanocortin-4 receptor (hMC4R)Inhibition of binding to human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL327479	211294	0	None	-	0	Mouse	7.2	pEC50	=	7.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL2369970	209751	0	None	-	0	Mouse	6.2	pEC50	=	6.2	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		11828678	207873	0	None	-	0	Mouse	6.2	pEC50	=	6.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	721	16	8	6	1.0	CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm0104872
		CHEMBL96531	207873	0	None	-	0	Mouse	6.2	pEC50	=	6.2	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL	721	16	8	6	1.0	CC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)CCc2ccccc2C1	10.1021/jm0104872
		CHEMBL2369962	209743	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		44269214	98494	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	546	12	3	6	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL276012	98494	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	546	12	3	6	3.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](O)Cc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL152986	208797	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccccc1)C(N)=O	10.1021/jm020296e
		CHEMBL358833	211803	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(N)=O)C(c1ccccc1)c1ccccc1	10.1021/jm020296e
		CHEMBL190551	209066	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190732	209067	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL2371829	210134	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Effective concentration against human melanocortin receptor-4 expressed in 293 HEK cellsEffective concentration against human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL3354723	211549	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL3354723	211549	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmc.2014.09.055
		CHEMBL349795	211720	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1cccs1)C(N)=O	10.1021/jm020296e
		CHEMBL3354740	211556	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Displacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assayDisplacement of Eu-DTPA-NDP-a-MSH chelate from human melanocortin-4 receptor expressed in HEK293 cells after 1 hr by competitive DELFIA assay	ChEMBL		None	None	None		CC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2014.09.055
		11813437	98529	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	530	12	2	5	4.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL276301	98529	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	In vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cellsIn vitro effective concentration towards human Melanocortin 4 receptor (MC4R) was determined by a SPA-based cAMP assay in melanoma cells	ChEMBL	530	12	2	5	4.0	CCCC(=O)C1(c2ccccc2)CCN(C(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)CCc2c[nH]cn2)CC1	10.1021/jm025600i
		CHEMBL2096693	209204	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/jm020296e
		CHEMBL2369977	209758	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Effective concentration for mouse Melanocortin-4 receptorEffective concentration for mouse Melanocortin-4 receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)N([C@@H](Cc2ccc(O)cc2)C(N)=O)[C@@](C)(C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049010r
		CHEMBL2371147	210017	0	None	-	0	Mouse	5.1	pEC50	=	5.1	Binding	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cellsActivity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@]1(C(N)=O)CCc2ccccc2C1	10.1021/jm020296e
		CHEMBL317969	211208	0	None	-	0	Mouse	6.1	pEC50	=	6.1	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		44308666	168862	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1890	64	23	21	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		91932723	168862	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1890	64	23	21	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL438160	168862	0	None	-	0	Human	8.1	pEC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cellsBinding affinity towards human melanocortin 4 receptor was determined using [125I]-NDP-alpha-MSH as radioligand transfected in HEK293 human embryonic kidney cells	ChEMBL	1890	64	23	21	-0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCOCCOCCNC(=O)CCC(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O	10.1016/j.bmcl.2003.09.079
		CHEMBL330561	211333	0	None	-	0	Mouse	7.0	pEC50	=	7.0	Binding	In vitro activation of mouse recombinant Melanocortin-4 receptor.In vitro activation of mouse recombinant Melanocortin-4 receptor.	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cccs1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm0104872
		CHEMBL2096742	209206	0	None	5	2	Human	10.2	pIC50	=	10.2	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0202526
		CHEMBL1161322	208508	0	None	1	2	Human	10.1	pIC50	=	10.1	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		6918780	63467	1	None	-	0	Human	10.0	pIC50	=	10	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL179836	63467	1	None	-	0	Human	10.0	pIC50	=	10	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		1324	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		16154396	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		16197727	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		44285019	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		57514683	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		91898441	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		CHEMBL441738	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		DB04931	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.11.014
		1324	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		16154396	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		16197727	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		44285019	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		57514683	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		91898441	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		CHEMBL441738	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		DB04931	302	25	None	-3	4	Human	9.8	pIC50	=	9.8	Binding	Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells	ChEMBL		None	None	None		None	10.1016/j.bmc.2016.03.006
		CHEMBL1161323	208509	0	None	5	2	Human	9.8	pIC50	=	9.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O	10.1021/jm0202526
		122194229	123983	0	None	-	1	Human	9.8	pIC50	=	9.8	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		CHEMBL3629347	123983	0	None	-	1	Human	9.8	pIC50	=	9.8	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		1324	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		16154396	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		16197727	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		44285019	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		57514683	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		91898441	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		CHEMBL441738	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		DB04931	302	25	None	-3	4	Human	9.7	pIC50	=	9.7	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.bmc.2013.03.016
		72548703	161567	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
		CHEMBL4128926	161567	0	None	-	0	Human	9.7	pIC50	=	9.7	Binding	Displacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]NDP-alpha -MSH from human recombinant MC4 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
		44366081	10262	0	None	2	2	Human	9.6	pIC50	=	9.6	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		CHEMBL1161313	10262	0	None	2	2	Human	9.6	pIC50	=	9.6	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		CHEMBL2369484	209627	0	None	-	0	Mouse	9.6	pIC50	=	9.6	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		11061068	31292	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		CHEMBL140154	31292	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		11061068	31292	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
		CHEMBL140154	31292	0	None	-	0	Human	9.5	pIC50	=	9.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm025539h
		10304547	168252	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL433764	168252	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		1324	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16154396	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16197727	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		44285019	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		57514683	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		91898441	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL441738	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		DB04931	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		1324	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		16154396	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		16197727	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		44285019	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		57514683	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		91898441	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		CHEMBL441738	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		DB04931	302	25	None	-3	4	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm030111j
		50899078	18154	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269573	18154	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	5	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		16746823	18157	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269576	18157	0	None	-	0	Human	9.4	pIC50	=	9.4	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	679	6	0	6	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CC(N(C)C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1161318	208505	0	None	79	2	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O	10.1021/jm0202526
		1324	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16154396	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16197727	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		44285019	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		57514683	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		91898441	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		CHEMBL441738	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		DB04931	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		44366171	121294	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm0202526
		CHEMBL358015	121294	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm0202526
		16725559	94989	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254757	94989	0	None	-	0	Rat	9.3	pIC50	=	9.3	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		122184910	122555	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601428	122555	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		10864861	115200	4	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL334457	115200	4	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL1161316	208504	0	None	63	2	Human	9.3	pIC50	=	9.3	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O	10.1021/jm0202526
		1324	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16154396	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16197727	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		44285019	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		57514683	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		91898441	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		CHEMBL441738	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		DB04931	302	25	None	-3	4	Human	9.3	pIC50	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		56659456	63701	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801215	63701	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](O)C1	10.1016/j.bmcl.2010.06.062
		44397455	123843	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL362523	123843	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3CC2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL2096742	209206	0	None	5	2	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm801300c
		CHEMBL500743	214124	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		1338	3807	43	None	-	4	Rat	9.2	pIC50	=	9.2	Binding	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		9938402	3807	43	None	-	4	Rat	9.2	pIC50	=	9.2	Binding	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL339053	3807	43	None	-	4	Rat	9.2	pIC50	=	9.2	Binding	Evaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against rat Melanocortin-4 receptor (rMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		44408154	141362	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
		CHEMBL383719	141362	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	668	8	2	5	5.1	CC1(C)CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)S1(=O)=O	10.1016/j.bmcl.2005.11.095
		44417552	141578	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL384955	141578	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		56673302	63671	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801095	63671	0	None	-	0	Human	9.2	pIC50	=	9.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		1323	2688	55	None	-10	3	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		92432	2688	55	None	-10	3	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		CHEMBL430239	2688	55	None	-10	3	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		6918849	122964	1	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL360818	122964	1	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	620	7	3	4	5.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2CCc3ccccc3[C@@H]2N)CC1	10.1016/j.bmcl.2005.05.012
		54587278	60818	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	587	6	3	4	4.7	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1762009	60818	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	587	6	3	4	4.7	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		44408286	140668	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		CHEMBL381501	140668	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	634	8	2	5	5.5	CC1(C)COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		16746686	18156	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269575	18156	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	651	5	0	6	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		44441641	94301	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL250508	94301	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	603	8	2	7	4.0	Cn1nnnc1CC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		56676638	63693	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801146	63693	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	0	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCOCC1	10.1016/j.bmcl.2010.06.062
		56666386	63702	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801216	63702	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	655	4	1	4	6.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL2115441	209268	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		49862736	15137	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209787	15137	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44408173	75401	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL203975	75401	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	640	8	2	5	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCCS2(=O)=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL2369484	209627	0	None	-	0	Mouse	9.0	pIC50	=	9.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		24857886	155248	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL402769	155248	0	None	-	0	Rat	9.0	pIC50	=	9	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		49862748	15149	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209799	15149	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	0	6	5.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCOCC1	10.1016/j.bmcl.2010.06.068
		CHEMBL393075	212462	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1016/j.bmcl.2007.02.020
		1323	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm070461w
		92432	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm070461w
		CHEMBL430239	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm070461w
		1324	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		16154396	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		16197727	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		44285019	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		57514683	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		91898441	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		CHEMBL441738	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		DB04931	302	25	None	-	4	Mouse	9.0	pIC50	=	9.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01894
		10304776	78979	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	6.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL2113041	78979	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	6.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCCc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		10282847	122965	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	5.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL360819	122965	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	634	7	3	4	5.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2CCc3ccccc3[C@@]2(C)N)CC1	10.1016/j.bmcl.2005.05.012
		1323	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
		92432	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
		CHEMBL430239	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b01285
		56669819	63691	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801144	63691	0	None	-	0	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	4	0	3	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC1	10.1016/j.bmcl.2010.06.062
		1323	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
		92432	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
		CHEMBL430239	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00488
		1323	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm060768f
		92432	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm060768f
		CHEMBL430239	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm060768f
		1323	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm801300c
		92432	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm801300c
		CHEMBL430239	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm801300c
		1323	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0510326
		92432	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0510326
		CHEMBL430239	2688	55	None	-10	3	Human	9.0	pIC50	=	9.0	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0510326
		1324	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		16154396	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		16197727	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		44285019	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		57514683	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		91898441	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		CHEMBL441738	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		DB04931	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		None	10.1021/jm960840h
		1324	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		16154396	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		16197727	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		44285019	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		57514683	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		91898441	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		CHEMBL441738	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		DB04931	302	25	None	-3	4	Human	8.9	pIC50	=	8.9	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1021/jm960845e
		1338	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.05.012
		9938402	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.05.012
		CHEMBL339053	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.05.012
		44358565	30026	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
		CHEMBL138901	30026	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	8	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCc2ccccc2N1	10.1016/j.bmcl.2003.09.026
		1338	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
		9938402	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
		CHEMBL339053	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.11.095
		44418431	136556	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
		CHEMBL373821	136556	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	334	4	0	2	3.1	O=C(Cc1ccccc1)N1C[C@@H]2CCCN2C[C@H]1Cc1ccccc1	10.1016/j.bmcl.2006.07.015
		CHEMBL503229	214163	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
		1338	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		9938402	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL339053	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		1338	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		9938402	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL339053	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		11017471	31917	0	None	-	1	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
		CHEMBL140738	31917	0	None	-	1	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm025539h
		1338	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		9938402	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL339053	3807	43	None	53	4	Human	8.9	pIC50	=	8.9	Binding	Evaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against human Melanocortin-4 receptor (hMC4R) by displacing [125I]NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm025539h
		CHEMBL443071	213920	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		CHEMBL1161321	208507	0	None	19	2	Human	8.9	pIC50	=	8.9	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1021/jm0202526
		1324	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16154396	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16197727	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		44285019	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		57514683	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		91898441	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		CHEMBL441738	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		DB04931	302	25	None	-	4	Mouse	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		44408287	75386	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		CHEMBL203911	75386	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		52943061	18148	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269568	18148	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		56683301	63697	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801150	63697	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@H](F)C1	10.1016/j.bmcl.2010.06.062
		56662904	63703	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801217	63703	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		49862750	15152	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209801	15152	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	657	5	1	6	5.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CC[C@H](O)C1	10.1016/j.bmcl.2010.06.068
		44349223	113800	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	673	11	0	7	3.7	CCOC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL332443	113800	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	673	11	0	7	3.7	CCOC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3348530	211402	0	None	-	0	Human	8.9	pIC50	=	8.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1016/j.bmcl.2003.10.056
		44310344	97329	0	None	-	0	Mouse	8.8	pIC50	=	8.8	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231883	97329	0	None	-	0	Mouse	8.8	pIC50	=	8.8	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL269274	97329	0	None	-	0	Mouse	8.8	pIC50	=	8.8	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		44347840	161924	0	None	17	3	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0202526
		91932630	161924	0	None	17	3	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0202526
		CHEMBL415333	161924	0	None	17	3	Human	8.8	pIC50	=	8.8	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0202526
		44448631	95070	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL255286	95070	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL501592	214141	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		15953833	78974	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113037	78974	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		15953833	78974	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113037	78974	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		56669820	63694	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
		CHEMBL1801147	63694	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	4	0	4	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1C[C@@H]2C[C@H]1CO2	10.1016/j.bmcl.2010.06.062
		56676639	63696	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801149	63696	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC[C@@H](F)C1	10.1016/j.bmcl.2010.06.062
		49862749	15151	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209800	15151	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	641	5	0	5	6.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCCC1	10.1016/j.bmcl.2010.06.068
		44448629	167463	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL429854	167463	0	None	-	0	Rat	8.8	pIC50	=	8.8	Binding	Binding affinity to rat MC4RBinding affinity to rat MC4R	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		52941830	18155	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		CHEMBL1269574	18155	0	None	-	0	Human	8.8	pIC50	=	8.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	637	4	0	5	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CCN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)c1ncnn1C	10.1016/j.bmcl.2010.09.049
		56659468	63692	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801145	63692	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	661	4	0	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		56679968	63695	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801148	63695	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	639	4	0	3	7.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCCC1	10.1016/j.bmcl.2010.06.062
		1323	2688	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
		92432	2688	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
		CHEMBL430239	2688	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.015
		CHEMBL385976	212371	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)N(CCCCN=C(N)N)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL2096742	209206	0	None	5	2	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm070461w
		CHEMBL266417	210683	0	None	8	3	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
		10210964	67243	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	606	7	3	4	5.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		CHEMBL187990	67243	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Concentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cellsConcentration required for 50% inhibition by displacement of of [125I]NDP-alpha-MSH of human MC4R expressed in CHO cells	ChEMBL	606	7	3	4	5.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C2N)CC1	10.1016/j.bmcl.2005.05.012
		132938008	159513	0	None	17	3	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4102048	159513	0	None	17	3	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		52945472	18149	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269569	18149	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		44357786	116754	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL337571	116754	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	514	10	2	6	3.5	CNCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10119206	118776	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL341982	118776	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	10	1	6	3.8	CN(C)CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		1324	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16154396	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		16197727	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		44285019	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		57514683	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		91898441	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		CHEMBL441738	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		DB04931	302	25	None	-3	4	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.9b00860
		145994283	167378	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	680	14	5	5	2.9	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4294862	167378	0	None	-	0	Human	8.0	pIC50	=	8	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	680	14	5	5	2.9	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL2373991	210381	0	None	5	2	Mouse	8.0	pIC50	=	8	Binding	Displacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 ReceptorDisplacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		CC[C@@H]1NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](CC(=O)O)NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/jm049620r
		127047336	139798	0	None	-1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3798768	139798	0	None	-1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1730	54	21	19	1.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423463	85396	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226281	85396	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		127047624	139896	0	None	1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3799408	139896	0	None	1	3	Mouse	8.0	pIC50	=	8.0	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1054	36	12	13	-0.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		145972289	164520	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4214826	164520	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		122184635	122434	0	None	-1	4	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600916	122434	0	None	-1	4	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44457043	97612	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL270923	97612	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	883	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		44423467	85421	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	584	10	0	4	7.1	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(C)(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226391	85421	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	584	10	0	4	7.1	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(C)(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44383343	120342	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21	10.1021/jm0309452
		CHEMBL353007	120342	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21	10.1021/jm0309452
		44397653	66992	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL186876	66992	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397445	123632	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(C(F)(F)F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361881	123632	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(C(F)(F)F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL425591	213338	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0510326
		71456236	78890	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2112918	78890	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	814	24	10	9	-0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		155546131	173530	0	None	-2	3	Mouse	6.0	pIC50	=	6	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4531291	173530	0	None	-2	3	Mouse	6.0	pIC50	=	6	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL190732	209067	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL2371963	210160	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm0614275
		44397337	67382	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188720	67382	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL203760	209161	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm0510326
		44373317	119658	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL346930	119658	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	787	22	9	9	0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1csc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		155551202	173959	0	None	-	0	Mouse	5.0	pIC50	=	5	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4541505	173959	0	None	-	0	Mouse	5.0	pIC50	=	5	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44417554	168839	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	867	15	10	9	-0.7	CC(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)N(CCCCN=C(N)N)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL437899	168839	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	867	15	10	9	-0.7	CC(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)N(CCCCN=C(N)N)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		44448477	95557	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257615	95557	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		122184576	122428	0	None	-	1	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600837	122428	0	None	-	1	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		155561116	174973	0	None	1	4	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4566163	174973	0	None	1	4	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44310259	161700	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932914	161700	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL413465	161700	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		10123761	99493	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determinedBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determined	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		CHEMBL283214	99493	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determinedBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH; not determined	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		44423430	85234	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225693	85234	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL3600921	211824	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44361027	31294	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm049278i
		CHEMBL140155	31294	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm049278i
		44361027	31294	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		CHEMBL140155	31294	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	600	8	3	6	2.5	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@@H](N)Cc3c[nH]cn3)CC2)c2ccccc21	10.1021/jm025539h
		10232394	119178	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	599	13	2	7	3.3	CN(C)CCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL343076	119178	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	599	13	2	7	3.3	CN(C)CCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10483153	60811	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761873	60811	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL501642	214142	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		44397410	124359	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL363740	124359	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349224	16548	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	10	0	6	3.1	CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL123744	16548	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	10	0	6	3.1	CC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		10145026	12269	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184727	12269	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028962	12269	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)C1CNC[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)N1	10.1016/j.bmcl.2005.02.068
		44448590	95599	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257759	95599	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		10239507	85280	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226025	85280	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423457	85367	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226176	85367	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		49862739	15141	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209791	15141	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	583	6	0	4	7.3	CCC(CC)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		44357528	118276	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	680	14	1	6	6.9	O=C(CCN(Cc1ccccc1)Cc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL340959	118276	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	680	14	1	6	6.9	O=C(CCN(Cc1ccccc1)Cc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		71461649	78954	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113007	78954	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	629	11	1	6	3.6	CCN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL410795	212842	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		CHEMBL397413	212504	6	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1016/j.bmcl.2007.04.001
		44397535	172775	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL451249	172775	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44348200	160196	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		CHEMBL410949	160196	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1511	33	16	22	-1.7	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		122184575	122427	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600836	122427	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44441647	154690	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL399714	154690	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	631	8	2	7	4.1	Cn1nnnc1CC1(c2ccc(Cl)cc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL264190	210608	1	None	-	2	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
		9917301	85425	2	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226443	85425	2	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10973172	169281	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL441342	169281	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		44423428	85232	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225691	85232	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44358915	13077	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1190181	13077	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL540320	13077	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		10146090	28045	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	639	13	2	7	4.2	O=C(CCN1CCCCC1)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL137273	28045	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	639	13	2	7	4.2	O=C(CCN1CCCCC1)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10165866	119005	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	542	10	2	6	3.4	CC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL342590	119005	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	542	10	2	6	3.4	CC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44357167	168518	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL435400	168518	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL2386882	210394	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity to MC4R in HEK293 cellsBinding affinity to MC4R in HEK293 cells	ChEMBL		None	None	None		C#CCCC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCC)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1016/j.bmcl.2013.02.022
		56673304	63680	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801120	63680	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	4	1	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)C	10.1016/j.bmcl.2010.06.062
		56669817	63682	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801122	63682	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	6	1	3	8.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCc1ccccc1	10.1016/j.bmcl.2010.06.062
		54584302	60812	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761874	60812	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@H](C)N1	10.1016/j.bmcl.2011.02.090
		10098971	124024	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL362985	124024	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		56658412	65912	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3573	117	45	45	-3.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCC(=O)NCCCC(CCCNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930590	65912	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3573	117	45	45	-3.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCC(=O)NCCCC(CCCNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835942	65912	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3573	117	45	45	-3.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCC(=O)NCCCC(CCCNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		71454491	78953	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113006	78953	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	615	10	1	6	3.2	CN1CCC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2005.01.060
		44373197	119473	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL345234	119473	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	800	23	10	9	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44422999	168855	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL	1040	15	9	10	3.0	CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		CHEMBL438118	168855	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL	1040	15	9	10	3.0	CCCC[C@H](NC(C)=O)C(=O)C[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		CHEMBL264190	210608	1	None	39	2	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		4189	206922	96	None	-46	34	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL1559	206922	96	None	-46	34	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL91	206922	96	None	-46	34	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		44358566	164883	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL422109	164883	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	10	2	7	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423426	143607	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389957	143607	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL1172251	208583	0	None	-	4	Human	5.9	pIC50	=	5.9	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		168278924	191066	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5187368	191066	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		10952071	31230	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL140108	31230	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@@H]1Cc2ccccc2CN1	10.1021/jm025539h
		44448436	95602	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257770	95602	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	577	6	1	3	6.6	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2cc(F)c(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		9919056	141069	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
		CHEMBL382511	141069	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	848	22	9	7	2.5	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccccc2)CC1	10.1016/j.bmcl.2005.08.012
		10210972	12275	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL1184771	12275	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145454	12275	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	607	9	3	5	3.5	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN(CC(F)F)CCN2)CC1	10.1016/j.bmcl.2004.10.020
		132180598	157849	0	None	-	1	Mouse	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4083717	157849	0	None	-	1	Mouse	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	803	17	10	7	-0.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		11753695	8393	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1093304	8393	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		10077258	15031	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209253	15031	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		11753695	8393	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093304	8393	7	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44397412	67311	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188395	67311	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349469	17093	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125492	17093	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	11	1	4	5.6	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccc2F)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		44448661	94999	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254792	94999	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		44441681	94129	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL249319	94129	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		44358660	168559	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL435697	168559	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL544851	168559	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		49862376	15040	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209319	15040	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		44397702	124085	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL363280	124085	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	10	2	8	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccsc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44358660	168559	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL435697	168559	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL544851	168559	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349026	117000	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	2	6	2.9	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCNCC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338811	117000	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	2	6	2.9	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CCNCC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3754655	212223	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.5b01285
		CHEMBL1172251	208583	0	None	-	4	Human	5.9	pIC50	=	5.9	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		71459937	78975	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113038	78975	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2371928	210154	0	None	-	0	Human	4.9	pIC50	=	4.9	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2006.07.036
		22318631	85252	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	532	10	1	5	5.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(O)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225965	85252	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	532	10	1	5	5.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(O)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423437	136836	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	504	9	0	4	5.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Cl)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL374176	136836	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	504	9	0	4	5.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Cl)cc2)CC1	10.1016/j.bmc.2006.12.039
		155561116	174973	0	None	-1	4	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4566163	174973	0	None	-1	4	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	964	11	11	11	-1.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		122184578	122430	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600839	122430	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		137651071	157467	0	None	-	1	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4079298	157467	0	None	-	1	Mouse	6.9	pIC50	=	6.9	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	794	15	7	6	1.3	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		176	398	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2157	398	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2566	398	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		CHEMBL633	398	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		DB01118	398	66	None	-6	31	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		122184577	122429	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600838	122429	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1102	17	12	11	0.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600834	211815	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44357527	118894	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	590	12	2	6	5.0	O=C(CCNCc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL342268	118894	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	590	12	2	6	5.0	O=C(CCNCc1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44447251	154798	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
		CHEMBL400237	154798	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	531	5	0	4	5.4	CC(C)(C)N1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2CCC(CN3CCOC3=O)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2007.11.128
		56661897	65916	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2821	85	36	36	-2.5	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930594	65916	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2821	85	36	36	-2.5	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835946	65916	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2821	85	36	36	-2.5	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL2331674	209532	0	None	-	1	Human	7.9	pIC50	=	7.9	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)(NC(=O)CNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(=O)NCCC(N)=O)nn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml300312b
		1324	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16154396	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16197727	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		44285019	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		57514683	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		91898441	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		CHEMBL441738	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		DB04931	302	25	None	-3	4	Human	7.9	pIC50	=	7.9	Binding	Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		44396987	67193	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		CHEMBL187774	67193	0	None	-	0	Human	7.9	pIC50	=	7.9	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		44423384	12857	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188648	12857	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL536977	12857	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccc(F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		2247	505	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		249	505	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		2603	505	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		CHEMBL296419	505	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		DB00637	505	81	None	-147	42	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		155532232	171705	0	None	2	3	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4466724	171705	0	None	2	3	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44358698	30924	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL139803	30924	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	574	8	2	7	5.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)N[C@@H]3CCc4ccccc4NC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423432	85236	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	10	0	4	5.4	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225749	85236	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	10	0	4	5.4	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		44441634	94011	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	478	6	2	4	3.6	CC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248700	94011	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	478	6	2	4	3.6	CC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		131839615	212636	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16133835	212636	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		CHEMBL407070	212636	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		44275263	161926	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		CHEMBL415341	161926	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1022	13	11	9	1.5	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		10077258	15031	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209253	15031	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	596	8	0	5	4.5	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		49862664	15123	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209706	15123	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	513	3	1	4	5.4	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44423460	85380	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226228	85380	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL186970	209054	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		44277696	101205	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
		CHEMBL29582	101205	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/j.bmcl.2005.08.012
		10373417	100805	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		CHEMBL29317	100805	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		44277696	101205	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
		CHEMBL29582	101205	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)00830-2
		49862426	15061	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209383	15061	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	6	0	4	4.6	CC(=O)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)C(C)C	10.1016/j.bmcl.2010.06.038
		10973172	169281	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL441342	169281	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	502	8	0	5	4.4	CC(CN1CCN(CC(c2ccc(Cl)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL203170	209158	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC1=O	10.1021/jm0510326
		44372933	119913	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL349298	119913	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	770	22	10	8	-0.7	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		49862744	15145	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209795	15145	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		11730771	15256	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		CHEMBL12120	15256	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		10481801	16857	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12487	16857	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		2726	919	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		621	919	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		83	919	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL71	919	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		DB00477	919	68	None	-154	72	Human	4.8	pIC50	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		44423452	85311	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(-c4ccccc4)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226073	85311	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(-c4ccccc4)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		155551202	173959	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4541505	173959	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	895	8	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL1172249	208582	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172253	208585	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL190080	209062	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190953	209077	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL2371835	210137	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		49798107	10846	0	None	-	2	Human	5.8	pIC50	=	5.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933502	10846	0	None	-	2	Human	5.8	pIC50	=	5.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172247	10846	0	None	-	2	Human	5.8	pIC50	=	5.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		44423440	85243	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Br)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225854	85243	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(Br)cc2)CC1	10.1016/j.bmc.2006.12.039
		10128451	116147	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	512	8	2	6	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)C1CNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL335779	116147	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	512	8	2	6	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)C1CNC1	10.1016/j.bmcl.2003.09.036
		10141778	116719	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL337351	116719	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	500	9	2	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		131839615	212636	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16133835	212636	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		CHEMBL407070	212636	26	None	1	2	Human	7.8	pIC50	=	7.8	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		6918813	131371	3	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL368876	131371	3	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		54584301	60810	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
		CHEMBL1761872	60810	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	585	6	2	4	4.6	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1C	10.1016/j.bmcl.2011.02.090
		71452720	78971	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		CHEMBL2113031	78971	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		52944242	18153	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269572	18153	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	609	4	1	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1cnn[nH]1	10.1016/j.bmcl.2010.09.049
		CHEMBL204864	209166	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCC)NC1=O	10.1021/jm0510326
		CHEMBL3600832	211813	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44441639	94050	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248893	94050	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	532	7	2	4	4.8	N#CCC1(C2CCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		9842665	156806	12	None	-3	2	Human	6.8	pIC50	=	6.8	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
		CHEMBL40711	156806	12	None	-3	2	Human	6.8	pIC50	=	6.8	Binding	Binding affinity at MC4RBinding affinity at MC4R	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmc.2008.03.072
		CHEMBL1172249	208582	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172253	208585	0	None	-	4	Human	6.8	pIC50	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		145977650	163834	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4206406	163834	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	865	11	12	9	-0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL2371966	210163	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm0614275
		24774358	154904	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	811	9	10	8	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL400866	154904	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	811	9	10	8	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		44397460	126219	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365004	126219	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44396125	66284	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	374	5	1	2	4.8	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.08.055
		CHEMBL184736	66284	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	374	5	1	2	4.8	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.08.055
		CHEMBL2371973	210170	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(Cc3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/jm0614275
		CHEMBL375947	212232	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		44441685	94132	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL249322	94132	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	585	7	3	5	3.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCC(C)(C)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		10481801	16857	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12487	16857	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	9	0	5	5.0	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCCC3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44397700	67324	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc4ccccc4c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188451	67324	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc4ccccc4c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2096759	209208	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44401323	11800	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1181891	11800	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028961	11800	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	569	7	4	5	3.1	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNC3(CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44448698	94932	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254351	94932	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL409144	212747	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CC(=O)O)NC1=O	10.1021/jm0510326
		CHEMBL446185	213944	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0510326
		CHEMBL3600913	211822	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44431513	145809	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1054	14	12	10	1.4	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		CHEMBL391704	145809	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1054	14	12	10	1.4	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		44348183	97165	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1493	31	14	21	-0.8	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL268094	97165	0	None	-	0	Human	4.8	pIC50	=	4.8	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1493	31	14	21	-0.8	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		44441638	154380	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	504	7	2	4	4.0	N#CCC1(C2CC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL398717	154380	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	504	7	2	4	4.0	N#CCC1(C2CC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44441683	94130	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL249320	94130	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	543	8	3	5	2.5	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CCC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		44423431	85235	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CCCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225748	85235	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CCCN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10951027	16842	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL12480	16842	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		122184912	122558	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601430	122558	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44357294	28202	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	4.0	CC(C)(N)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL137367	28202	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	4.0	CC(C)(N)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		71449119	78968	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL2113028	78968	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	643	7	3	6	4.2	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CNCCN2C(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2004.10.020
		49862375	15039	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209318	15039	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		49862377	15041	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209320	15041	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		168273822	190570	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5180152	190570	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		44423449	85279	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	10	0	5	6.1	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226024	85279	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	10	0	5	6.1	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		71456245	78976	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113039	78976	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		122184499	122393	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1088	17	13	11	0.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600737	122393	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1088	17	13	11	0.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44423378	12841	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188561	12841	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL536747	12841	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3c(F)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44357547	28122	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	596	10	2	6	3.9	O=C(CCNC(=O)C(F)(F)F)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL137318	28122	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	596	10	2	6	3.9	O=C(CCNC(=O)C(F)(F)F)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL413573	213075	0	None	-	2	Human	6.8	pIC50	=	6.8	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
		44396126	66113	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	404	5	1	2	5.6	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nc(C)c[nH]1	10.1016/j.bmcl.2004.08.055
		CHEMBL183954	66113	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	404	5	1	2	5.6	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nc(C)c[nH]1	10.1016/j.bmcl.2004.08.055
		44423450	85278	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	9	0	4	5.4	CC(C)N1CCN(C(CN2CCN(CCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226023	85278	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	514	9	0	4	5.4	CC(C)N1CCN(C(CN2CCN(CCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423427	85431	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226502	85431	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		122184909	122554	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601427	122554	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		11092574	18810	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		CHEMBL12783	18810	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		131839615	212636	26	None	1	2	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16133835	212636	26	None	1	2	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		CHEMBL407070	212636	26	None	1	2	Human	7.7	pIC50	=	7.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/s0960-894x(03)00164-1
		16132144	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		16133793	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		44273719	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		CHEMBL214332	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2004.10.020
		16132144	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		16133793	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		44273719	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		CHEMBL214332	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.05.109
		44397660	123431	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361731	123431	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	618	11	2	8	5.5	COc1ccc([C@H]2CNC[C@@H]2C(=O)N[C@H](C)CCc2cc(Sc3ccc(Cl)cc3)nn(-c3ccc(OC)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349228	18815	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL127861	18815	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	538	9	0	4	4.4	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		16132144	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		16133793	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		44273719	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		CHEMBL214332	209279	36	None	-30	4	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsInhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2005.02.068
		24764421	13180	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	527	10	0	3	6.9	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1190957	13180	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	527	10	0	3	6.9	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL541897	13180	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	527	10	0	3	6.9	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		16721030	12903	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188987	12903	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL537873	12903	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL373344	212175	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		44358630	28314	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL137452	28314	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL541866	28314	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL3752534	212216	1	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C1=O	10.1021/acs.jmedchem.5b01285
		CHEMBL417853	213238	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- agouti related protein (AGRP) as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		155536962	172237	0	None	1	2	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4474215	172237	0	None	1	2	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		10008561	15016	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209192	15016	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	588	10	0	4	6.5	CC(C)CN(CC(C)C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL417853	213238	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibitory activity against hMC4R (human melanocortin receptor) using I-AGRP as radioligandInhibitory activity against hMC4R (human melanocortin receptor) using I-AGRP as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		10928744	16792	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL12457	16792	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		155536962	172237	0	None	-1	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4474215	172237	0	None	-1	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	923	9	8	10	-0.6	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CS)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44358609	28779	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL137855	28779	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1172619	208588	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL408509	212720	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		CHEMBL364711	212032	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		1323	2688	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
		92432	2688	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
		CHEMBL430239	2688	55	None	-10	3	Human	8.7	pIC50	=	8.7	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00114-8
		1324	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		16154396	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		16197727	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		44285019	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		57514683	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		91898441	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		CHEMBL441738	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		DB04931	302	25	None	-	4	Mouse	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.7b00301
		56679956	63700	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801214	63700	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	675	4	0	3	7.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.062
		46919520	15138	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209788	15138	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	597	4	0	5	6.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44349471	16873	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL124954	16873	0	None	-	1	Human	8.7	pIC50	=	8.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL410217	212808	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		56683299	63689	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801142	63689	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	0	3	7.3	CCN(C)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		145980838	166666	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	670	14	5	5	3.1	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4281687	166666	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	670	14	5	5	3.1	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@@H]1CCCN1C(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		44408155	140553	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
		CHEMBL381125	140553	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	656	10	2	5	4.9	CC(C)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.11.095
		56676632	63678	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801118	63678	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		44358639	29991	1	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	526	8	2	7	3.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NC3CCCCNC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL138878	29991	1	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	526	8	2	7	3.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NC3CCCCNC3=O)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		56676614	63704	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801218	63704	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	0	4	7.1	CO[C@H]1CCN(C(=O)C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)C1	10.1016/j.bmcl.2010.06.062
		1323	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/ml500436s
		92432	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/ml500436s
		CHEMBL430239	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL		None	None	None		None	10.1021/ml500436s
		1323	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
		92432	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
		CHEMBL430239	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		None	10.1016/j.bmcl.2011.03.019
		1323	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
		92432	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
		CHEMBL430239	2688	55	None	-10	3	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		None	10.1016/j.ejmech.2018.04.021
		49862747	15148	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209798	15148	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	6	1	5	6.1	CCNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL3600736	211812	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		49862745	15146	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
		CHEMBL1209796	15146	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	615	5	0	5	6.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N(C)C	10.1016/j.bmcl.2010.06.068
		49862751	15153	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209802	15153	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	677	5	0	5	6.8	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)N1CCC(F)(F)C1	10.1016/j.bmcl.2010.06.068
		44397569	122906	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL360602	122906	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		56676631	63669	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801093	63669	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		56676635	63687	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801127	63687	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	669	5	1	4	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC1CCOCC1	10.1016/j.bmcl.2010.06.062
		CHEMBL502300	214152	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		CHEMBL428801	213472	0	None	-3	3	Human	8.6	pIC50	=	8.6	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm00018a005
		CHEMBL365913	212043	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		56659466	63673	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801097	63673	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		56673305	63683	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
		CHEMBL1801123	63683	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	631	6	1	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCF	10.1016/j.bmcl.2010.06.062
		56659467	63686	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
		CHEMBL1801126	63686	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	629	6	2	4	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCCO	10.1016/j.bmcl.2010.06.062
		56683300	63690	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801143	63690	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	0	3	7.7	CCN(CC)C(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		49862665	15124	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209707	15124	0	None	-	0	Human	8.6	pIC50	=	8.6	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	5	1	5	5.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)CO)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44391929	12412	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1185810	12412	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145453	12412	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	571	8	3	5	3.3	CCN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL414778	213156	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44401315	12281	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184825	12281	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028957	12281	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		10123761	99493	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		CHEMBL283214	99493	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	898	21	9	7	2.1	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(Br)cccc2C1	10.1016/s0960-894x(02)00830-2
		CHEMBL1172619	208588	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		118735101	118801	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421678	118801	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	824	15	9	6	2.4	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(Br)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		118735103	118803	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421680	118803	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	698	15	8	9	-0.8	CC(=O)N[C@H]1Cn2nncc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		11757528	15017	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209193	15017	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	10	0	4	6.0	CCCN(CCC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		44397654	67188	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL187761	67188	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		155532232	171705	0	None	-2	3	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4466724	171705	0	None	-2	3	Mouse	5.7	pIC50	=	5.7	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	992	12	11	11	-1.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44431512	145924	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		CHEMBL391796	145924	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPalphaMSH from human MC4R expressed in HEK293 cells	ChEMBL	1038	14	12	10	0.9	CCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)N2Cc3ccccc3CC(NC1=O)C2=O	10.1016/j.bmcl.2007.02.020
		127053937	149053	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	502	11	2	4	4.3	CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O	nan
		CHEMBL3942822	149053	0	None	-	0	Human	4.7	pIC50	=	4.7	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	502	11	2	4	4.3	CCC(CC)CN1CC[C@H](CNC(=O)/C=C/c2ccc(Cl)cc2)N[C@H](CCN2CCCCC2)C1=O	nan
		122184633	122432	0	None	-	1	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600914	122432	0	None	-	1	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		44358693	13059	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1190075	13059	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL540077	13059	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423422	85424	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226442	85424	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	8	0	4	4.5	CN1CCN(C(CN2CCN(CCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL432895	213635	4	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
		44357406	119275	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	572	12	2	7	3.0	COCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL343742	119275	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	572	12	2	7	3.0	COCC(=O)NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		127046262	139820	0	None	1	3	Mouse	7.7	pIC50	=	7.7	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3798912	139820	0	None	1	3	Mouse	7.7	pIC50	=	7.7	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1012	35	12	13	-0.3	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44390411	63896	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL180487	63896	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	609	8	2	6	2.8	CN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL417853	213238	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- NDP-MSH as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		CHEMBL264190	210608	1	None	39	2	Mouse	6.7	pIC50	=	6.7	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		10874535	16521	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		CHEMBL12369	16521	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		16725558	155669	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL404905	155669	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		10004020	18848	2	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12811	18848	2	None	-	0	Human	6.7	pIC50	=	6.7	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44358669	13827	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC(C)CNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1195769	13827	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC(C)CNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL555316	13827	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC(C)CNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423424	85427	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CN1CCN(C(CN2CCN(CCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226496	85427	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	502	10	0	4	5.3	CN1CCN(C(CN2CCN(CCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44357280	27661	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL136993	27661	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44357626	119274	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	9	2	6	4.0	O=C(C[C@@H]1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL343720	119274	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	9	2	6	4.0	O=C(C[C@@H]1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		22318636	85253	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	12	0	5	6.5	CC(C)Oc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225966	85253	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	12	0	5	6.5	CC(C)Oc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		10098971	124024	0	None	-	1	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL362985	124024	0	None	-	1	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		71459938	78981	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113043	78981	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptorInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		71459938	78981	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113043	78981	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		44373198	52166	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL158808	52166	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	848	22	10	8	0.1	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44441636	94012	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248701	94012	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	520	9	2	4	4.8	CCCCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44448554	155372	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403421	155372	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		56668797	65911	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3609	108	42	48	-3.2	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930589	65911	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3609	108	42	48	-3.2	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835941	65911	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3609	108	42	48	-3.2	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		132180599	156893	0	None	-	1	Mouse	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4072129	156893	0	None	-	1	Mouse	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	841	20	11	7	0.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/acs.jmedchem.7b00301
		118735102	118802	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421679	118802	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	707	15	8	6	1.1	CC(=O)N[C@H]1Cc2ccccc2CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		44349226	116983	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338747	116983	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	601	10	1	6	2.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCNCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3349030	211405	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		155566718	175916	0	None	3	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4587214	175916	0	None	3	2	Human	4.7	pIC50	=	4.7	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44358697	12962	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1189383	12962	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL538589	12962	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44423442	85246	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	538	9	0	4	5.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225909	85246	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	538	9	0	4	5.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423468	83473	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	604	11	0	4	7.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL220092	83473	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	604	11	0	4	7.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423445	85251	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc(CCCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)c2ccccc12	10.1016/j.bmc.2006.12.039
		CHEMBL225964	85251	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc(CCCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)c2ccccc12	10.1016/j.bmc.2006.12.039
		49862378	15042	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209321	15042	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		44423454	85327	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226123	85327	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cccc(F)c3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL508501	214942	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		44423382	13948	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1196602	13948	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL557585	13948	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44423462	85395	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226280	85395	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3cccc(F)c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2372623	210277	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		44423438	85240	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2Br)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225800	85240	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2Br)CC1	10.1016/j.bmc.2006.12.039
		11050211	34822	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		CHEMBL143131	34822	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		11050211	34822	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL143131	34822	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	589	8	3	6	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cc2nnn[nH]2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		44401321	11796	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1181867	11796	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028960	11796	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44423459	85379	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226227	85379	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1cccc(-c2ccccc2)c1CCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		44423433	85426	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	556	10	0	4	6.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CCCCC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL226444	85426	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	556	10	0	4	6.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C3CCCCC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		44423453	85312	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226074	85312	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	528	10	0	4	5.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(-c4ccccc4)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL3600842	211819	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		11092487	162588	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL416890	162588	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44357348	119339	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL344231	119339	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	611	11	3	7	3.4	O=C(CCNC(=O)[C@@H]1CCCNC1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		10373417	100805	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		CHEMBL29317	100805	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Binding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSHBinding affinity towards human melanocortin receptor hMC4R by using radioligand NDP-MSH	ChEMBL	863	22	9	8	1.4	CCCCC(=O)NC1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CCc2c(cccc2N(C)C)C1	10.1016/s0960-894x(02)00830-2
		6918780	63467	1	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		CHEMBL179836	63467	1	None	-	0	Human	7.6	pIC50	=	7.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	637	10	2	6	3.6	CCCN(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.01.060
		90661465	77162	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
		CHEMBL2028958	77162	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
		CHEMBL2078649	77162	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	693	9	5	6	4.0	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C3CC3)CN2)CC1.CC(F)(F)C(=O)O	10.1016/j.bmcl.2005.02.068
		155548853	173809	0	None	3	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4538274	173809	0	None	3	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL427205	213352	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0510326
		CHEMBL1172252	208584	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL2372623	210277	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL188738	209059	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL191120	209080	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL3799094	212268	0	None	-	0	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL103817	208459	0	None	1	3	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423446	138152	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	12	0	5	6.1	CCOc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL376829	138152	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	560	12	0	5	6.1	CCOc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		15953833	78974	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113037	78974	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL1172252	208584	0	None	-	4	Human	6.6	pIC50	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		133053557	163706	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4204975	163706	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	851	11	12	9	-1.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		10098568	15018	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209194	15018	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	532	8	0	4	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		22318671	85247	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	515	10	0	6	4.7	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225910	85247	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	515	10	0	6	4.7	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmc.2006.12.039
		10951027	16842	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		CHEMBL12480	16842	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	486	8	0	5	3.9	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)cc1	10.1021/jm0255522
		49862425	15060	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209382	15060	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		44423456	85331	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226125	85331	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423458	85368	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3c(Cl)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226177	85368	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3c(Cl)cccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL1161320	208506	0	None	-12	2	Human	6.6	pIC50	=	6.6	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O	10.1021/jm0202526
		CHEMBL526334	215681	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm801300c
		CHEMBL263822	210590	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
		155546131	173530	0	None	2	3	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4531291	173530	0	None	2	3	Human	5.6	pIC50	=	5.6	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	929	9	8	10	-0.4	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL381739	212292	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0510326
		137653916	158580	0	None	-	1	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4091894	158580	0	None	-	1	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	828	18	9	8	1.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL2096710	209205	0	None	-	1	Mouse	6.6	pIC50	=	6.6	Binding	Displacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 ReceptorDisplacement of [125I]-hAGRP(87-132) from mouse Melanocortin 4 Receptor	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm049620r
		44358608	30295	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL139126	30295	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCCNC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		10257242	15030	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209252	15030	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		10188529	126781	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		CHEMBL365401	126781	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@H]2CC[C@@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		44397659	67119	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL187450	67119	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397534	67268	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188142	67268	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397338	123677	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL362129	123677	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@H]3CNCC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44448515	155444	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403834	155444	0	None	-	0	Human	7.6	pIC50	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		44390422	63468	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL179837	63468	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	644	10	1	5	5.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		71459937	78975	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113038	78975	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CCNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		11092487	162588	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL416890	162588	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	514	9	0	5	4.8	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(c3ccccc3)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		10257242	15030	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209252	15030	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	560	7	0	4	5.1	CC(=O)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		44390424	63927	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180635	63927	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2ccc3ncccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		44401319	12282	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184826	12282	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028959	12282	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44310103	166647	0	None	2	2	Mouse	7.5	pIC50	=	7.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231882	166647	0	None	2	2	Mouse	7.5	pIC50	=	7.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL428134	166647	0	None	2	2	Mouse	7.5	pIC50	=	7.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		44397339	67474	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@@H]3CNCC[C@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL189236	67474	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	11	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC[C@@H]3CNCC[C@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2369485	209628	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		127047913	139924	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3799563	139924	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	962	35	12	13	-1.5	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)COCC(=O)NCCCOCCOCCOCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423441	85244	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	484	9	0	4	5.1	Cc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225855	85244	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	484	9	0	4	5.1	Cc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		44358917	13038	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1189954	13038	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL539813	13038	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL217305	209373	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	10.1016/s0960-894x(03)00412-8
		44349221	96497	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	655	12	0	6	4.0	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(CC3CC3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL262512	96497	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	655	12	0	6	4.0	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(CC3CC3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		11273288	12960	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL1189370	12960	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL538567	12960	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		44401520	13930	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1196472	13930	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL557154	13930	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		56662925	63676	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801116	63676	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		101880965	161954	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		44426646	161954	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		91971099	161954	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL415660	161954	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1698	53	23	21	-3.3	C#CCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmcl.2007.04.001
		44397409	122944	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL360717	122944	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		1324	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		16154396	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		16197727	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		44285019	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		57514683	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		91898441	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		CHEMBL441738	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		DB04931	302	25	None	-3	4	Human	8.5	pIC50	=	8.5	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		44426648	167588	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	4166	145	50	54	2.3	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn2cc(CCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(=O)O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		91971095	167588	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	4166	145	50	54	2.3	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn2cc(CCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(=O)O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL430079	167588	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	4166	145	50	54	2.3	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn2cc(CCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(=O)O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		16725559	94989	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254757	94989	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.5	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		44349222	113799	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	701	10	0	7	4.5	CC(C)(C)OC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL332442	113799	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	701	10	0	7	4.5	CC(C)(C)OC(=O)N1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		71449047	78480	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2111807	78480	0	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2372588	210272	0	None	316	2	Human	8.5	pIC50	=	8.5	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O	10.1021/jm0202526
		44441643	154800	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL400252	154800	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	591	8	2	7	3.9	Cn1nnnc1CC1(CC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		49862746	15147	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209797	15147	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	5	1	5	5.7	CNC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		1324	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		16154396	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		16197727	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		44285019	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		57514683	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		91898441	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		CHEMBL441738	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		DB04931	302	25	None	-3	4	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against human Melanocortin 4 receptorInhibitory activity against human Melanocortin 4 receptor	ChEMBL		None	None	None		None	10.1021/jm00018a005
		CHEMBL2372589	210273	0	None	-15	2	Human	8.4	pIC50	=	8.4	Binding	Binding affinity against human Melanocortin-4 receptorBinding affinity against human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1021/jm0202526
		44441644	154838	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL400456	154838	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CCC(C)C1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44397444	123635	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361890	123635	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	6.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C(F)(F)F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44426647	143009	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2342	83	28	30	3.6	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		91971098	143009	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2342	83	28	30	3.6	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL389469	143009	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2342	83	28	30	3.6	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1cn(CCCCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		56662927	63688	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
		CHEMBL1801141	63688	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	657	6	2	4	6.7	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)(C)CO	10.1016/j.bmcl.2010.06.062
		122184637	122436	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600918	122436	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		10230144	30395	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	3.8	CC(C)(CN)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL139217	30395	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	528	9	2	6	3.8	CC(C)(CN)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		44391940	12250	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1184624	12250	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145456	12250	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	614	8	4	6	2.1	C[C@H](N)C(=O)N1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		73345549	89451	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2371218	89451	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44445085	97074	0	None	-	2	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	879	9	11	9	1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL267265	97074	0	None	-	2	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	879	9	11	9	1.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		11215758	66079	0	None	125	3	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration against Melanocortin 4 receptorInhibitory concentration against Melanocortin 4 receptor	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183799	66079	0	None	125	3	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration against Melanocortin 4 receptorInhibitory concentration against Melanocortin 4 receptor	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		44372964	51747	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL158471	51747	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.3	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		1337	3424	6	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	3424	6	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	3424	6	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		1337	3424	6	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	3424	6	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	3424	6	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		22318657	85233	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	9	1	4	4.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCNCC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225692	85233	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	474	9	1	4	4.6	Fc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCNCC2)cc1	10.1016/j.bmc.2006.12.039
		122184911	122556	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601429	122556	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1130	17	10	11	1.5	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		1016	3747	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2561	3747	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2733526	3747	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		5384	3747	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		CHEMBL83	3747	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		DB00675	3747	78	None	-70	35	Human	4.5	pIC50	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		10886436	119157	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		CHEMBL342954	119157	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Evaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cellsEvaluated for binding affinity against Melanocortin-4 receptor by displacing [125I]-NDP-alpha-MSH radioligand expressed in CHO cells	ChEMBL	588	8	2	6	4.6	O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm025539h
		49862662	15121	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209704	15121	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	569	3	0	4	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1172246	208581	0	None	-	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O	10.1016/j.bmcl.2010.05.078
		56682297	65918	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2033	62	26	26	-2.3	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930595	65918	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2033	62	26	26	-2.3	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835948	65918	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2033	62	26	26	-2.3	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		10098133	15015	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209191	15015	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	518	7	1	4	4.9	CC(C)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL417853	213238	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligandBinding affinity against human melanocortin 4 receptor (hMC4R) using [125I]- ([Nle4]alpha-MSH) as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		CHEMBL417853	213238	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibitory activity against hMC4R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligandInhibitory activity against hMC4R (human melanocortin receptor) using [125I]-[Nle4] alpha-MSH as radioligand	ChEMBL		None	None	None		C[C@H](c1ccccc1)N(CC(N)=O)C(=O)CN(C(=O)CNCCCN=C(N)N)C(c1ccccc1)c1ccccc1	10.1016/s0960-894x(03)00164-1
		44310242	156309	0	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932912	156309	0	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL406550	156309	0	None	-	0	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		122184914	122559	0	None	-	1	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3601432	122559	0	None	-	1	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1144	17	9	11	1.8	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL191063	209079	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		CHEMBL372237	212172	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL189991	209061	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12	10.1021/jm0490033
		44441648	154691	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL399715	154691	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	8	2	8	2.9	Cn1nnnc1CC1(C2CCOCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL1172246	208581	0	None	-	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O	10.1016/j.bmcl.2010.05.078
		44349470	16933	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125308	16933	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	589	11	1	5	4.9	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NCc2ccccn2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		155544852	174939	0	None	1	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4565367	174939	0	None	1	4	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL3600841	211818	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		145966716	164305	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4212209	164305	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	887	11	12	9	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL2370695	209912	0	None	2	2	Mouse	5.5	pIC50	=	5.5	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		10928744	16792	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL12457	16792	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	466	9	0	5	3.6	CCN1CCN(C(CN2CCN(CC(C)C(=O)c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		11016325	16526	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	480	6	0	5	3.7	CN1CCN(C(CN2CCN(CC3CCc4ccccc4C3=O)CC2)c2ccc(Cl)cc2)CC1	10.1021/jm0255522
		CHEMBL12370	16526	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	480	6	0	5	3.7	CN1CCN(C(CN2CCN(CC3CCc4ccccc4C3=O)CC2)c2ccc(Cl)cc2)CC1	10.1021/jm0255522
		57854192	153049	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	576	11	5	4	4.2	N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O	nan
		CHEMBL3975851	153049	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	576	11	5	4	4.2	N=C(N)NCCC[C@H]1N[C@@H](CNC(=O)c2ccc3ccccc3c2)CCN(CC(c2ccccc2)c2ccccc2)C1=O	nan
		15953838	67270	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL188146	67270	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL539306	67270	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL4299619	213595	0	None	-	0	Mouse	7.5	pIC50	=	7.5	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44423455	85328	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226124	85328	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL194552	209099	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		15953838	67270	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188146	67270	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL539306	67270	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44445083	154305	0	None	-	1	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	953	9	10	9	2.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL398665	154305	0	None	-	1	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	953	9	10	9	2.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)CCCNCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		91971097	115268	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1381	51	15	16	6.7	CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmcl.2007.04.001
		CHEMBL3348561	115268	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	1381	51	15	16	6.7	CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmcl.2007.04.001
		44347927	157276	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1443	31	14	21	-1.9	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL407680	157276	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1443	31	14	21	-1.9	CC(=O)[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL1201469	14507	0	None	-2	4	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		None	nan
		44423359	13894	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	487	9	0	3	6.0	CN1CCC(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1196208	13894	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	487	9	0	3	6.0	CN1CCC(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL556164	13894	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	487	9	0	3	6.0	CN1CCC(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44423429	137215	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL375057	137215	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3ccc4ccccc4c3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		11733360	98376	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL275299	98376	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44358705	96625	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL263461	96625	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CCNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL383250	212312	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0510326
		49798104	10845	0	None	-	3	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172244	10845	0	None	-	3	Human	6.5	pIC50	=	6.5	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		9808720	64222	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180892	64222	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		44423425	143606	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CN1CCN(C(CN2CCN(CCCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389956	143606	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	11	0	4	5.7	CN1CCN(C(CN2CCN(CCCCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44441689	154418	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL398932	154418	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	569	7	3	6	1.8	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CC(=O)CC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		127053935	144185	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	602	11	2	4	6.2	O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1	nan
		CHEMBL3904191	144185	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	602	11	2	4	6.2	O=C(NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCCN2CCCCC2)N1)c1ccc2ccccc2c1	nan
		49862376	15040	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209319	15040	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1ncccn1	10.1016/j.bmcl.2010.06.038
		10122170	130319	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	638	10	3	7	2.2	CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL368008	130319	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	638	10	3	7	2.2	CS(=O)(=O)N(CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2310901	209498	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		73350149	89453	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2371220	89453	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	820	22	10	8	0.5	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		6918707	104192	1	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	104192	1	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL264190	210608	1	None	-	2	Human	6.5	pIC50	=	6.5	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		22318643	85248	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	485	9	1	5	4.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(N)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225911	85248	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	485	9	1	5	4.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(N)cc2)CC1	10.1016/j.bmc.2006.12.039
		44397651	66951	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL186675	66951	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	670	10	2	7	7.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3Cl)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44441687	94005	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL248671	94005	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.3	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3(C)CCCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		44423461	85394	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226279	85394	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44423444	138120	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	594	10	0	4	6.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(Br)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL376609	138120	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	594	10	0	4	6.4	CC(C)N1CCN(C(CN2CCN(CCCCc3c(Br)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL227239	209451	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2cc3ccccc3s2)N(CC)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		11092574	18810	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		CHEMBL12783	18810	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.6	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(Cl)c(Cl)c1	10.1021/jm0255522
		44448628	155117	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL402009	155117	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	571	7	1	4	6.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(OC)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		145976444	163963	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4207858	163963	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	889	11	12	9	-0.1	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		71456219	78747	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2112603	78747	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		71456220	78748	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1483	33	16	22	-2.5	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL2112604	78748	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1483	33	16	22	-2.5	CC(=O)[C@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		155548853	173809	0	None	-3	4	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4538274	173809	0	None	-3	4	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	1005	13	10	10	-0.6	CC(C)[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL263948	210599	1	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960840h
		16132144	209279	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		16133793	209279	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		44273719	209279	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		CHEMBL214332	209279	36	None	-30	4	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm960845e
		44358630	28314	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL137452	28314	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL541866	28314	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		11811937	17970	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	424	8	0	4	3.4	CN1CCN(C(CN2CCN(CCCc3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL12615	17970	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	424	8	0	4	3.4	CN1CCN(C(CN2CCN(CCCc3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1021/jm0255522
		CHEMBL444493	213933	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		46884748	8396	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093307	8396	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44397459	125794	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364789	125794	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	11	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44358633	13843	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(C(C)CCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1195894	13843	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(C(C)CCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL555546	13843	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(C(C)CCNC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		49798104	10845	0	None	-	3	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172244	10845	0	None	-	3	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1381	39	14	13	3.5	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCC(=O)N(c1ccccc1)C1CCN(CCc2ccccc2)CC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		49798108	10847	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933501	10847	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172248	10847	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL370321	212167	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL371610	212170	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		44441645	94127	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL249277	94127	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	605	12	2	7	4.4	CCCCCCC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44408190	96923	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL265985	96923	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	606	8	2	5	4.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCOC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		44448629	167463	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL429854	167463	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL2371712	210109	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		73354641	89452	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2371219	89452	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	838	22	10	8	0.6	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		44401522	12784	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1188041	12784	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL534928	12784	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	4	5	3.5	CC(C)[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		44448631	95070	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL255286	95070	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	6	1	3	7.0	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(Br)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		44417551	141443	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		CHEMBL384166	141443	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	846	15	9	10	0.0	CC(=O)N[C@H]1CSSC[C@@H](C(=O)N(CCCCN=C(N)N)[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm060768f
		1324	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		16154396	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		16197727	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		44285019	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		57514683	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		91898441	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		CHEMBL441738	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		DB04931	302	25	None	-	4	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determinedInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined	ChEMBL		None	None	None		None	10.1021/jm0303608
		11215553	8394	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093305	8394	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44408189	168879	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
		CHEMBL438259	168879	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	619	8	2	4	4.6	CN1CCN(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1=O	10.1016/j.bmcl.2005.11.095
		44349593	118389	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL341055	118389	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	705	11	0	6	4.4	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)c3ccccc3)CC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		44310344	97329	0	None	-	0	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231883	97329	0	None	-	0	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL269274	97329	0	None	-	0	Mouse	8.4	pIC50	=	8.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4414	53	53	68	-9.9	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)NN(Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		11215553	8394	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1093305	8394	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		44408275	75419	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		CHEMBL204078	75419	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	620	8	2	5	5.1	C[C@H]1COC(=O)N1CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.11.095
		44408276	75507	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL204308	75507	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	632	8	2	5	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		9808801	60809	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761871	60809	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		44397356	66917	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL186557	66917	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CN(C)CC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397698	126201	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364992	126201	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	10	2	7	6.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3ccc(C)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44310103	166647	0	None	2	2	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		77231882	166647	0	None	2	2	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		CHEMBL428134	166647	0	None	2	2	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	4237	51	50	66	-10.2	CC(=O)NN[C@H]1CSSSSC[C@@H]2NC(=O)[C@@H]3CSSSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)C(N)=O)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H](Cc5ccc(O)cc5)NC(=O)[C@H](CSSSSC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc5c[nH]cn5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C(C)C)NC1=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC2=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N4	10.1021/jm0303608
		44408252	140669	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL381503	140669	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	605	8	3	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2CCNC2=O)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		44349247	116989	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	671	13	0	6	4.6	CC(C)CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338767	116989	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	671	13	0	6	4.6	CC(C)CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		52918026	60808	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1761870	60808	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	571	6	3	4	4.2	C[C@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](C)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL2386883	210395	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity to MC4R in HEK293 cellsBinding affinity to MC4R in HEK293 cells	ChEMBL		None	None	None		C#CCCC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2013.02.022
		44401313	12287	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1184856	12287	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL2028956	12287	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	571	8	4	5	3.3	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		22318635	13990	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	11	0	4	6.8	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)C2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1196957	13990	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	11	0	4	6.8	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)C2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL558789	13990	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	11	0	4	6.8	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)C2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2007.01.019
		579	3144	18	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.036
		6918468	3144	18	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.036
		CHEMBL41547	3144	18	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL		None	None	None		None	10.1016/j.bmcl.2006.07.036
		44426652	166456	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2243	81	24	26	8.5	CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmcl.2007.04.001
		91971096	166456	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2243	81	24	26	8.5	CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmcl.2007.04.001
		CHEMBL427795	166456	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	2243	81	24	26	8.5	CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCCCn1cc(CCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmcl.2007.04.001
		49798107	10846	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933502	10846	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172247	10846	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1358	22	17	18	-1.3	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		44348144	157822	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL408336	157822	0	None	-	0	Human	4.4	pIC50	=	4.4	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1533	33	16	22	-1.3	CC(=O)C1CSSCC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		10348630	30196	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL139042	30196	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(C)NC(=O)[C@H]3CNCC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		44396986	67432	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		CHEMBL188966	67432	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	568	7	3	4	4.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H]2C[C@H]3CC[C@@H]2NC3)CC1	10.1016/j.bmcl.2005.05.109
		44423465	85407	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL226342	85407	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	10	0	4	6.1	Cc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		44275312	141407	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		CHEMBL384036	141407	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		56661653	65613	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	4071	117	45	54	-5.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930588	65613	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	4071	117	45	54	-5.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1833974	65613	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	4071	117	45	54	-5.9	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		44390421	63906	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180544	63906	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.01.060
		44310243	169187	0	None	-	0	Mouse	5.4	pIC50	=	5.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932909	169187	0	None	-	0	Mouse	5.4	pIC50	=	5.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL440633	169187	0	None	-	0	Mouse	5.4	pIC50	=	5.4	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		44423466	166332	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL427270	166332	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	558	11	0	5	5.8	COc1ccc(-c2ccccc2CCCN2CCN(CC(c3ccc(F)cc3)N3CCN(C(C)C)CC3)CC2)cc1	10.1016/j.bmc.2006.12.039
		10213106	72426	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
		CHEMBL198772	72426	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Binding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacementBinding affinity towards human Melanocortin 4 receptor using radiolabeled NDP-MSH displacement	ChEMBL	892	24	9	8	2.9	CCCCC(=O)N[C@]1(C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(N)=O)CC[C@H](c2ccc(OCC)cc2)CC1	10.1016/j.bmcl.2005.08.012
		137649368	157406	0	None	-	1	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4078495	157406	0	None	-	1	Mouse	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	844	15	7	6	2.4	CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		44397570	122909	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL360603	122909	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(Cl)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL3349030	211405	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		24774519	94854	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	911	9	10	8	2.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL253788	94854	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	911	9	10	8	2.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		71456246	78978	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113040	78978	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		145964837	164347	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4212629	164347	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	875	11	12	9	-0.5	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		49862740	15142	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		CHEMBL1209792	15142	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	6	0	5	6.1	COCC(C)N1C[C@@H](C(=O)N2CCC3(CC2)O[C@H](C(C)(C)C#N)c2cc(C)c(Cl)cc23)[C@H](c2ccc(F)cc2F)C1	10.1016/j.bmcl.2010.06.068
		49798108	10847	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		91933501	10847	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172248	10847	0	None	-	2	Human	6.4	pIC50	=	6.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL	1408	22	17	18	-0.1	Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N1CC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CSSC[C@@H](N)C1=O	10.1016/j.bmcl.2010.05.078
		118735099	118799	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421676	118799	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	746	15	9	6	1.6	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		44397655	67307	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188360	67307	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	627	10	2	8	5.7	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(C#N)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44397658	125426	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364582	125426	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	10	2	7	6.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		1334	1501	7	None	-1	3	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16133814	1501	7	None	-1	3	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL437050	1501	7	None	-1	3	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL411359	212879	0	None	-	0	Human	7.4	pIC50	=	7.4	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		168274393	190105	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5172938	190105	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL376339	212244	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		137658359	159571	0	None	-	1	Mouse	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4102774	159571	0	None	-	1	Mouse	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	791	20	11	7	-1.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL2331673	209531	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assay	ChEMBL		None	None	None		CC(=O)NCC(=O)NC(CCCNC(=O)CCNC(=O)C(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)CCNC(=O)C(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1021/ml300312b
		49862478	15075	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209458	15075	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		44401585	13763	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL1195347	13763	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL554368	13763	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	585	8	3	5	3.6	CC[C@@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1C	10.1016/j.bmcl.2005.02.068
		CHEMBL264190	210608	1	None	-	2	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm2009937
		10864263	16412	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		CHEMBL12310	16412	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		56679964	63672	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801096	63672	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	599	4	1	3	6.6	CNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		44577510	188735	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
		CHEMBL504986	188735	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of [125I]-[Nle4, D-Phe7]alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	893	12	11	11	0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)c2cc([N+](=O)[O-])ccc2SC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701181n
		71456245	78976	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113039	78976	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		44423448	85255	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	572	11	0	5	6.2	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCC3)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225968	85255	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	572	11	0	5	6.2	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C3CCCC3)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2371965	210162	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2CC3CCCCC3N2C1=O	10.1021/jm0614275
		CHEMBL2371969	210166	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](C(C)C)NC1=O	10.1021/jm0614275
		49862663	15122	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209705	15122	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	613	3	0	5	7.0	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL438294	213766	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		CHEMBL2370695	209912	0	None	2	2	Mouse	5.3	pIC50	=	5.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		49862378	15042	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		CHEMBL1209321	15042	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	534	8	0	4	4.6	CC(=O)N(CC(CC(C)C)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)C	10.1016/j.bmcl.2010.06.038
		52943061	18148	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269568	18148	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	610	4	0	5	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)CC2C(C)(C)c1nnco1	10.1016/j.bmcl.2010.09.049
		44397411	126385	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365074	126385	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc(F)c3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		56672278	65917	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	1231	38	16	16	-2.4	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCC(=O)NC(CCCNC(C)=O)(CCCNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835947	65917	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	1231	38	16	16	-2.4	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCC(=O)NC(CCCNC(C)=O)(CCCNC(C)=O)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL2331675	209533	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells by time resolved fluorescence binding assay	ChEMBL		None	None	None		CC(=O)NCCCC(CCCNC(C)=O)(NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)nn1)C(=O)NCCC(N)=O	10.1021/ml300312b
		16132144	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		16133793	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		44273719	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		CHEMBL214332	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm049579s
		16132144	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		16133793	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		44273719	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		CHEMBL214332	209279	36	None	-30	4	Human	8.3	pIC50	=	8.3	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm030111j
		44401530	12795	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1188092	12795	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL535152	12795	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	597	8	4	5	3.7	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3(C)CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44401528	13989	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1196956	13989	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL558787	13989	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	599	7	4	5	3.9	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C(C)(C)C)CN2)CC1	10.1016/j.bmcl.2005.02.068
		54586246	60817	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		CHEMBL1762008	60817	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	599	8	3	4	5.0	CC[C@@H]1CN(C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C[C@@H](CC)N1	10.1016/j.bmcl.2011.02.090
		145975465	163949	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4207725	163949	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	825	11	12	9	-1.6	CC1(C)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		56683297	63685	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		CHEMBL1801125	63685	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		CHEMBL266288	96963	0	None	-	1	Mouse	8.3	pIC50	=	8.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	5507	70	67	87	-15.6	CSCC[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2CSSSSC[C@@H]3NC(=O)[C@@H]4CCCN4C(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]4CSSSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](CSSSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@@H]5CCCN5C(=O)[C@H](CC(N)=O)NC1=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CSSSSC[C@H](N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N4)NC3=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSSSC[C@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCN=C(N)N)NC1=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/jm0303608
		44358625	31199	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	535	11	1	7	5.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NCCOc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL140077	31199	0	None	-	0	Human	8.3	pIC50	=	8.3	Binding	Concentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4RConcentration required to inhibit binding of [125I]NDP-alpha-MSH from membranes prepared from CHO cells expressing human MC4R	ChEMBL	535	11	1	7	5.2	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CCC(=O)NCCOc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL524861	215623	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C1=O	10.1021/jm801300c
		52940633	18151	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269570	18151	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	624	4	0	5	7.5	Cc1nc(C(C)(C)C2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)no1	10.1016/j.bmcl.2010.09.049
		10030530	17599	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125819	17599	0	None	-	1	Human	8.2	pIC50	=	8.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL413226	213056	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)C	10.1016/j.bmcl.2007.04.001
		56683296	63679	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801119	63679	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	627	5	1	3	7.3	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NC(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL455070	213999	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		71452716	78893	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2112920	78893	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		6918707	104192	1	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	104192	1	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL1172428	208586	0	None	-	3	Human	6.3	pIC50	=	6.3	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL1172428	208586	0	None	-	3	Human	6.3	pIC50	=	6.3	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		CHEMBL365794	212041	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL2371828	210133	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)Cc1ccccc1)C(C)=O	10.1021/jm0490033
		CHEMBL2371833	210136	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL3600922	211825	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600843	211820	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		2683	102888	25	None	-676	16	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL305906	102888	25	None	-676	16	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL334255	102888	25	None	-676	16	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL1775066	208881	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1016/j.bmcl.2011.03.019
		44392015	12778	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1187982	12778	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL3216179	12778	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		10004020	18848	2	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL12811	18848	2	None	-	0	Human	7.3	pIC50	=	7.3	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	452	8	0	5	3.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44423376	12868	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1188733	12868	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL537208	12868	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3cc(F)ccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		44441646	154088	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL398487	154088	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	611	9	2	7	3.7	Cn1nnnc1CC1(Cc2ccccc2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		49862737	15139	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209789	15139	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	611	5	0	5	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(CC4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44423373	12773	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1187954	12773	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL534503	12773	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccc(F)cc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		24774521	154258	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL398635	154258	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)/C=C\C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		44448480	95558	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL257616	95558	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		56666397	63674	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801098	63674	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	5	1	3	7.0	CCNC(=O)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		145988152	167044	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4288909	167044	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	720	17	7	6	2.3	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(Br)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		49862478	15075	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		CHEMBL1209458	15075	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	7	0	5	4.0	CC(C)N(CC(N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(C)(C)C)S(C)(=O)=O	10.1016/j.bmcl.2010.06.038
		44423464	85406	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(Cl)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226341	85406	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	562	10	0	4	6.5	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(Cl)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		127047853	139993	0	None	-	0	Mouse	7.3	pIC50	=	7.3	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3799955	139993	0	None	-	0	Mouse	7.3	pIC50	=	7.3	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1948	72	23	25	-2.1	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		71459938	78981	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113043	78981	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2369485	209628	0	None	-	0	Mouse	6.3	pIC50	=	6.3	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NN[C@H]2Cc3ccc(O)cc3NC2=O)CC(=O)N[C@H](C(=O)NN[C@@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		122184634	122433	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600915	122433	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		56669816	63677	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		CHEMBL1801117	63677	0	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	625	5	1	3	7.1	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NC1CC1	10.1016/j.bmcl.2010.06.062
		71461652	78980	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113042	78980	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		44423439	85241	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(Br)c2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225801	85241	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	548	9	0	4	5.5	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(Br)c2)CC1	10.1016/j.bmc.2006.12.039
		44423421	143330	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389733	143330	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	460	7	0	4	4.1	CN1CCN(C(CN2CCN(CCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		168295131	192242	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5205283	192242	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccc(cc2)CSC(C)(C)[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		44396140	168220	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL433574	168220	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2371962	210159	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0614275
		44397633	126380	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365051	126380	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	636	10	2	7	6.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(Cl)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		5624	32693	14	None	-169	10	Human	4.2	pIC50	=	4.2	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL1203324	32693	14	None	-169	10	Human	4.2	pIC50	=	4.2	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL141343	32693	14	None	-169	10	Human	4.2	pIC50	=	4.2	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		11730771	15256	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		CHEMBL12120	15256	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	497	9	0	7	3.2	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc([N+](=O)[O-])cc1	10.1021/jm0255522
		56659465	63670	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801094	63670	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	6.9	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)N(C)C	10.1016/j.bmcl.2010.06.062
		145973779	164732	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	929	11	12	9	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4217528	164732	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	929	11	12	9	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL3600840	211817	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL389674	212433	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		44423420	85423	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226441	85423	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	446	6	0	4	4.1	CN1CCN(C(CN2CCN(Cc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10874535	16521	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		CHEMBL12369	16521	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	482	9	0	6	3.3	COc1ccc(C(=O)C(C)CN2CCN(CC(c3ccc(F)cc3)N3CCN(C)CC3)CC2)cc1	10.1021/jm0255522
		11733360	98376	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		CHEMBL275299	98376	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	In vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of alpha [125I]NDP-MSH to the human Melanocortin 4 receptor	ChEMBL	468	8	0	5	3.8	CC(CN1CCN(CC(c2cccc(Cl)c2)N2CCN(C)CC2)CC1)C(=O)c1ccccc1	10.1021/jm0255522
		44441642	154405	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL398816	154405	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	577	9	2	7	3.5	CC(C)CC1(Cc2nnnn2C)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44397220	167304	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		CHEMBL429387	167304	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	CN1C[C@@H]2CC[C@H]1[C@@H](C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC1)C2	10.1016/j.bmcl.2005.05.109
		CHEMBL413439	213070	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		CHEMBL438920	213809	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44401310	12785	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL1188043	12785	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		CHEMBL534930	12785	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	557	7	4	5	2.9	C[C@H]1CN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)CN1	10.1016/j.bmcl.2005.02.068
		44448660	94973	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL254589	94973	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		49862743	15144	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209794	15144	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	629	5	1	5	5.6	CC(=O)NC(C)(C)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL3600833	211814	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		118735100	118800	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		CHEMBL3421677	118800	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis	ChEMBL	764	15	9	6	1.8	CC(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C1=O	10.1021/ml500436s
		56676633	63681	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
		CHEMBL1801121	63681	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	641	6	1	3	7.6	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@@H]2C(C)(C)C(=O)NCC(C)C	10.1016/j.bmcl.2010.06.062
		49862738	15140	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		CHEMBL1209790	15140	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	555	4	0	4	6.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(F)cc3F)CC1)O[C@@H]2C(C)(C)C#N	10.1016/j.bmcl.2010.06.068
		44441684	94131	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL249321	94131	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	571	7	3	5	3.1	CC1CCC(C2(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc3ccc(F)cc3)NC(=O)[C@H]3CN(C)CCN3)CC2)CC1	10.1016/j.bmcl.2006.11.084
		44441633	94530	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL251735	94530	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	546	7	2	4	5.2	N#CCC1(C2CCCCC2)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44457067	97742	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL271586	97742	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	877	12	10	8	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		15603023	97964	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL272660	97964	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	849	12	10	8	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		44397657	124123	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL363384	124123	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	624	10	2	7	5.8	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3F)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		16157270	212553	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		CHEMBL405282	212553	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		16157270	212553	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		CHEMBL405282	212553	14	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm049579s
		CHEMBL380638	212271	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCC)NC1=O	10.1021/jm0510326
		73351850	89519	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL2373212	89519	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	781	22	9	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		127053936	152240	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	598	11	2	4	5.7	O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1	nan
		CHEMBL3968918	152240	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.Radioligand Binding Assay: Radioligand binding assays were carried out using commercial or in-house prepared hMC1R, hMC3R and hMC4R membranes and [125I] NDP-MSH, as per the hMC5R procedure in Example 102. In-house plasma membranes were prepared from transfected mammalian cells (prepared as in Example 109, using plasmid DNA containing the human MC1R, MC3R or MC4R gene or other gene of interest in a plasmid vector with a mammalian origin of replication): Adherent cells were washed with warm Hanks buffered saline solution (HBSS). 1 mL of cold HBSS was added to each flask and the cells were scraped off with a rubber policeman. The scraped cells were added to a 50 mL tube on ice. The plates were then rinsed twice with 5 mL cold HBSS and this was also added to the tube. The cells were centrifuged at 1000×g for 5 mins in a bench top centrifuge and the supernatant was decanted. The remaining cell pellet was resuspended in 0.25 M sucrose. The cell suspension was centrifuged again as previously and the pellet resuspended in 5 mL of 0.25 M sucrose containing protease inhibitors. The cells were homogenised by a 10 second pulse with an Ika disperser followed by 30 seconds on ice. The homogenisation and ice incubation was repeated three times. The mixture was then centrifuged at 1260×g for 5 mins. The supernatant was decanted into another centrifuge tube, to which a buffer containing 50 mM Tris, pH 7.4, 12.5 mM MgCl2, 5 mM EGTA and protease inhibitors was added to make the volume up to 30 mL. This was centrifuged at 30,000×g for 90 mins at 4° C. The resulting pellet was resuspended in 1 mL of the buffer above also containing 10% glycerol. Membranes were aliquoted into cryovials which were snap-frozen in a dry-ice/ethanol bath before being stored at −80° C. until required for use.	ChEMBL	598	11	2	4	5.7	O=C(/C=C/c1ccc(Cl)cc1)NC[C@H]1CCN(CC(c2ccccc2)c2ccccc2)C(=O)[C@@H](CCN2CCCCC2)N1	nan
		10146211	64329	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL181162	64329	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	649	10	2	6	3.6	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.01.060
		489667	59300	1	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	452	8	2	1	7.5	Cc1ccc2[nH]c(-c3ccc(Br)cc3)c(CCCCCNC3CCCCC3)c2c1	10.1021/jm0309452
		CHEMBL170530	59300	1	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition against human melanocortin-4 (MC4) receptorInhibition against human melanocortin-4 (MC4) receptor	ChEMBL	452	8	2	1	7.5	Cc1ccc2[nH]c(-c3ccc(Br)cc3)c(CCCCCNC3CCCCC3)c2c1	10.1021/jm0309452
		168282779	191171	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C	10.1021/acs.jmedchem.1c01848
		CHEMBL5188894	191171	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2ccccc2CSC1(C)C	10.1021/acs.jmedchem.1c01848
		49862377	15041	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209320	15041	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	654	9	0	6	6.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cnn(C(C)C)c1	10.1016/j.bmcl.2010.06.038
		44423469	85428	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	596	10	0	4	6.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226497	85428	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	596	10	0	4	6.8	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(C(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2369775	209686	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL		None	None	None		C#CCCC(=O)NCCCC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(C(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@@H]2CCCN2C(=O)CNCCCC(CCCNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC(=O)N2CCC[C@H]2C(=O)n2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@H](CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		168285801	191481	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
		CHEMBL5193501	191481	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1135	17	13	12	2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(N)=O)CSCc2cccc(c2)CSC1(C)C	10.1021/acs.jmedchem.1c01848
		44441637	94049	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL248892	94049	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	506	7	2	4	4.3	CC(C)C1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL188459	209057	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O)C(C)=O	10.1021/jm0490033
		CHEMBL1172429	208587	0	None	-	4	Human	6.2	pIC50	=	6.2	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		44441688	94354	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL250719	94354	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	555	7	3	5	2.6	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3C=CCCC3)CC2)C1	10.1016/j.bmcl.2006.11.084
		49862375	15039	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209318	15039	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	624	8	0	6	5.2	CC(C)N(CC(C1CCCCC1)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1)C(=O)c1cccnn1	10.1016/j.bmcl.2010.06.038
		CHEMBL439691	213848	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)ON	10.1021/jm049579s
		44449216	95271	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL256286	95271	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		145980719	166496	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4278563	166496	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	642	17	7	6	1.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL204310	209164	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/jm0510326
		44423451	85310	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	11	0	4	6.2	CC(C)N1CCN(C(CN2CCN(CCCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226072	85310	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	542	11	0	4	6.2	CC(C)N1CCN(C(CN2CCN(CCCCc3ccccc3-c3ccccc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL3600835	211816	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44391999	13909	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1196338	13909	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL3215542	13909	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		44423436	85239	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(F)c2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225799	85239	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	488	9	0	4	4.9	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2cccc(F)c2)CC1	10.1016/j.bmc.2006.12.039
		44397652	123634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL361883	123634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	620	10	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44349173	116990	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
		CHEMBL338768	116990	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	606	6	2	5	3.4	CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)c2ccccc21	10.1016/j.bmcl.2003.10.056
		44441686	97244	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL268722	97244	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	545	8	3	5	2.7	CCC(C)(C)C1(C(=O)NC(C)(C)C)CCN(C(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]2CN(C)CCN2)CC1	10.1016/j.bmcl.2006.11.084
		24848934	78952	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113004	78952	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	655	11	1	6	4.2	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2CN(C3CCCCC3)C2)CC1	10.1016/j.bmcl.2005.01.060
		155566718	175916	0	None	-3	2	Mouse	5.2	pIC50	=	5.2	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4587214	175916	0	None	-3	2	Mouse	5.2	pIC50	=	5.2	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	957	10	8	10	-0.5	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		44275312	141407	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		CHEMBL384036	141407	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligandBinding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand	ChEMBL	1023	13	11	9	1.9	CCCCC(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCc3c(Cl)cccc3C2)NC1=O	10.1016/s0960-894x(03)00114-8
		44310242	156309	0	None	-	0	Mouse	5.2	pIC50	=	5.2	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932912	156309	0	None	-	0	Mouse	5.2	pIC50	=	5.2	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL406550	156309	0	None	-	0	Mouse	5.2	pIC50	=	5.2	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		71461652	78980	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113042	78980	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	622	9	2	6	6.6	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNCC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		6918813	131371	3	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL368876	131371	3	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL509582	215546	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@H](NC(=N)N)CN2C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm801300c
		49862742	14970	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1208802	14970	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	601	4	0	5	6.1	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(Cl)cc21	10.1016/j.bmcl.2010.06.068
		1323	2688	55	None	-10	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
		92432	2688	55	None	-10	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
		CHEMBL430239	2688	55	None	-10	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c01848
		132938008	159513	0	None	-	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4102048	159513	0	None	-	3	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		49862741	15143	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
		CHEMBL1209793	15143	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	ChEMBL	585	4	0	5	5.6	CC(C)(C#N)[C@H]1OC2(CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(F)c(F)cc21	10.1016/j.bmcl.2010.06.068
		6918707	104192	1	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL309807	104192	1	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	601	14	5	4	3.7	CC(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCCNC(=N)N)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		24857886	155248	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL402769	155248	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	591	6	1	3	7.2	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2)CC1	10.1016/j.bmcl.2008.04.049
		44408388	140323	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		CHEMBL380635	140323	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	646	8	2	5	5.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(CN2C(=O)OCC23CCC3)(C2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.11.095
		44396140	168220	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL433574	168220	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Tested for inhibition of binding to MC4 receptorTested for inhibition of binding to MC4 receptor	ChEMBL	518	10	0	5	4.9	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3577981	211749	1	None	-	3	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL3577981	211749	1	None	29	3	Mouse	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		11555886	155634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
		CHEMBL404696	155634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.062
		11555886	155634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL404696	155634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		44397461	126227	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365005	126227	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	606	10	2	7	5.6	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		11555886	155634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
		CHEMBL404696	155634	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	559	6	1	3	6.4	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.09.049
		CHEMBL1172429	208587	0	None	-	4	Human	6.2	pIC50	=	6.2	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cellsDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1016/j.bmcl.2010.05.078
		1337	3424	6	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	3424	6	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	3424	6	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		56665372	65914	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3318	105	42	42	-3.5	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930592	65914	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3318	105	42	42	-3.5	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835944	65914	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3318	105	42	42	-3.5	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)Cn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		145967155	164243	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4211275	164243	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCC2)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL3350396	211479	0	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		22318639	137310	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	10	0	4	5.7	CC(C)N1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL375251	137310	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	516	10	0	4	5.7	CC(C)N1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL2371967	210164	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1021/jm0614275
		10146483	64178	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		CHEMBL180854	64178	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	671	10	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)Cc2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		122184636	122435	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600917	122435	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		56665373	65915	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2849	87	36	36	-1.8	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930593	65915	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2849	87	36	36	-1.8	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835945	65915	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	2849	87	36	36	-1.8	C#CCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CCC#C)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		145973975	164657	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4216654	164657	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	901	11	12	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL3349030	211405	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		10168556	63873	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		CHEMBL180366	63873	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	657	9	3	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)c2ccccc2)CC1)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.01.060
		44310259	161700	0	None	-	0	Mouse	5.1	pIC50	=	5.1	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932914	161700	0	None	-	0	Mouse	5.1	pIC50	=	5.1	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL413465	161700	0	None	-	0	Mouse	5.1	pIC50	=	5.1	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132)	ChEMBL	1421	24	20	20	-4.6	C[C@@H]1NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		145966490	164362	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4212762	164362	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	839	11	12	9	-1.2	CC1(C)NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL2371964	210161	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/jm0614275
		44423435	85237	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	470	9	0	4	4.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225750	85237	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	470	9	0	4	4.8	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccccc2)CC1	10.1016/j.bmc.2006.12.039
		44397458	67314	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	11	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL188404	67314	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	616	11	2	7	6.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CCNC[C@@H]3Cc3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44347838	96643	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1561	33	16	22	-0.6	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		CHEMBL263585	96643	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of human melanocortin 4 receptorInhibition of human melanocortin 4 receptor	ChEMBL	1561	33	16	22	-0.6	CC(=O)C1C(=O)N[C@H](CCC(=O)O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NC(C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)CSSC1(C)C	10.1021/jm030111j
		44423443	206375	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	6.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(-c3ccccc3)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL87552	206375	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	10	0	4	6.4	CN1CCN(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)c2ccc(-c3ccccc3)cc2)CC1	10.1016/j.bmc.2006.12.039
		44441635	167530	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	492	7	2	4	4.0	CCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		CHEMBL430015	167530	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	492	7	2	4	4.0	CCC1(CC#N)CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.11.084
		44448479	155371	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403420	155371	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	573	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2008.04.049
		1334	1501	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		16133814	1501	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL437050	1501	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	ChEMBL		None	None	None		None	10.1021/jm049579s
		CHEMBL204263	209163	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory activity against hMC4R transfected in HEK293 cellsInhibitory activity against hMC4R transfected in HEK293 cells	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](CCCN=C(N)N)NC1=O	10.1021/jm0510326
		CHEMBL217584	209377	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		1334	1501	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		16133814	1501	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		CHEMBL437050	1501	7	None	-1	3	Human	6.1	pIC50	=	6.1	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		None	10.1021/jm000211e
		24774356	94825	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL253574	94825	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	861	9	10	8	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)c2ccccc2C(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		71456246	78978	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL2113040	78978	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	608	9	2	6	6.2	COc1ccc(N2N=C(Sc3ccc(Cl)cc3)CC(CC[C@@H](C)NC(=O)[C@@H]3CNC[C@H]3c3ccc(F)cc3)C2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL3601426	211826	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL190551	209066	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CCc1c[nH]c2ccccc12)CC(=O)NCC(N)=O	10.1021/jm0490033
		CHEMBL190203	209064	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL190427	209065	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N(CCCCN)CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		CHEMBL275999	210826	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cellsDisplacement of [125I]NDP-MSH from human melanocortin receptor-4 expressed in 293 HEK cells	ChEMBL		None	None	None		CCCCN(CC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1ccccc1)C(=O)N(CCCN=C(N)N)CC(=O)N(CC(=O)NCC(N)=O)Cc1c[nH]c2ccccc12)C(C)=O	10.1021/jm0490033
		44391938	11746	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL1181567	11746	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL2145455	11746	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	599	9	3	5	3.9	CC(C)CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		6918813	131371	3	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		CHEMBL368876	131371	3	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCN[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)N2CCC(C(=O)NC(C)(C)C)(C3CCCCC3)CC2)C1	10.1016/j.bmcl.2004.10.020
		1337	3424	6	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	3424	6	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	3424	6	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		44401524	14006	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL1197052	14006	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		CHEMBL559181	14006	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nMInhibitory concentration to displace [125I]NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells; Control 19 nM	ChEMBL	583	8	4	5	3.3	CC(C)(C)NC(=O)C1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CN[C@@H](C3CC3)CN2)CC1	10.1016/j.bmcl.2005.02.068
		44408253	140344	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
		CHEMBL380727	140344	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	650	10	2	5	6.1	CCOC(=O)N(CC1(C2CCCCC2)CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1)C(C)C	10.1016/j.bmcl.2005.11.095
		10098971	124024	0	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL362985	124024	0	None	-	1	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmc.2006.12.039
		155544852	174939	0	None	-1	4	Mouse	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		CHEMBL4565367	174939	0	None	-1	4	Mouse	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting methodDisplacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	977	12	10	10	-0.5	CC(C)[C@@H]1NC(=O)[C@H](CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.9b00860
		46911588	63668	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		CHEMBL1801092	63668	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	613	4	0	3	7.0	CC(=O)N(C)C(C)(C)[C@@H]1CC2(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.06.062
		44349246	116988	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	12	0	6	4.0	CCCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL338766	116988	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	643	12	0	6	4.0	CCCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		44373177	119831	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		CHEMBL348511	119831	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cellsInhibitory concentration of compound was determined against hMC4R through displacement of NDP-MSH radioligand using HEK293 cells	ChEMBL	804	22	10	8	-0.0	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1016/s0960-894x(02)01052-1
		1337	3424	6	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		6918851	3424	6	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		CHEMBL364346	3424	6	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cellsInhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	ChEMBL	582	7	2	4	4.7	O=C([C@@H]1C[C@@H]2CC[C@H]1N(C2)C)N[C@@H](C(=O)N1CCC(CC1)(C1CCCCC1)C(=O)NC(C)(C)C)Cc1ccc(cc1)F	10.1016/j.bmcl.2005.05.109
		145964017	164041	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		CHEMBL4208874	164041	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting methodDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method	ChEMBL	915	11	12	9	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2(CCCCC2)NC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.8b00488
		44448677	155396	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL403556	155396	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	575	6	1	3	6.9	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(F)cc2Cl)CC1	10.1016/j.bmcl.2008.04.049
		44423447	85254	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	13	0	5	6.5	CCC(CC)N1CCN(C(CN2CCN(CCCCc3c(OC)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL225967	85254	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	574	13	0	5	6.5	CCC(CC)N1CCN(C(CN2CCN(CCCCc3c(OC)ccc4ccccc34)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		10864263	16412	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		CHEMBL12310	16412	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	In vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptorIn vitro ability to inhibit the binding of [125I]AGRP to the human Melanocortin 4 receptor	ChEMBL	520	8	0	5	4.3	CC(CN1CCN(CC(c2ccc(F)cc2)N2CCN(C)CC2)CC1)C(=O)c1ccc(C(F)(F)F)cc1	10.1021/jm0255522
		127046235	139638	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3797690	139638	0	None	-	0	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1004	36	12	13	-1.3	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(N)=O	10.1021/acs.jmedchem.5b01894
		132180597	156171	0	None	-	1	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4063911	156171	0	None	-	1	Mouse	7.1	pIC50	=	7.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	784	15	8	7	-0.0	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/acs.jmedchem.7b00301
		71454492	78955	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
		CHEMBL2113008	78955	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	643	13	1	6	3.9	CC(C)CCN1CC(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)C1	10.1016/j.bmcl.2005.01.060
		145990599	166855	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		CHEMBL4285535	166855	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysisDisplacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis	ChEMBL	710	17	7	6	2.6	CCCC[C@H](NC(=O)[C@@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.ejmech.2018.04.021
		44441682	154648	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL399474	154648	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	529	8	3	5	2.1	CN1CCN[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCC(CC3CC3)(C(=O)NC(C)(C)C)CC2)C1	10.1016/j.bmcl.2006.11.084
		CHEMBL2221249	209443	0	None	-4	3	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O	nan
		CHEMBL4299612	213594	0	None	-	0	Mouse	6.1	pIC50	=	6.1	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@@H]1C(=O)NCC(=O)N1CCC[C@H]1C(=O)NCC(N)=O	10.1021/acs.jmedchem.5b01894
		44423470	85429	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	612	11	0	5	6.7	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(OC(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL226498	85429	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	612	11	0	5	6.7	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(OC(F)(F)F)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		137653704	158633	0	None	-	1	Mouse	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4092424	158633	0	None	-	1	Mouse	6.1	pIC50	=	6.1	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	838	18	8	7	2.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		44391927	13991	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL1196971	13991	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
		CHEMBL3216393	13991	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligandConcentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	ChEMBL	557	7	3	5	2.9	CN1CCNC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N1CCC(C(=O)NC(C)(C)C)(C2CCCCC2)CC1	10.1016/j.bmcl.2004.10.020
		10117829	85245	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	500	10	0	5	4.8	COc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		CHEMBL225856	85245	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	500	10	0	5	4.8	COc1ccc(C(CN2CCN(CCCCc3cccc4ccccc34)CC2)N2CCN(C)CC2)cc1	10.1016/j.bmc.2006.12.039
		122184638	122437	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL3600919	122437	0	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL	1116	17	11	11	1.1	CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)N(C)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		56672277	65913	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3360	108	42	42	-2.4	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		91930591	65913	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3360	108	42	42	-2.4	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		CHEMBL1835943	65913	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assayDisplacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay	ChEMBL	3360	108	42	42	-2.4	C#CCCC(=O)NCCCCC(NC(C)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)Nc1cn(CCC(=O)NCCCC(CCCNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)(NC(=O)CNC(=O)CCn2cc(NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)C(CCCCNC(=O)CCC#C)NC(C)=O)nn2)C(=O)NCCC(N)=O)nn1	10.1021/jm2009937
		49862425	15060	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		CHEMBL1209382	15060	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in CHO cells	ChEMBL	570	9	0	5	4.0	CC(C)CC(CN(C(C)C)S(C)(=O)=O)N1CCN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)CC1	10.1016/j.bmcl.2010.06.038
		46884747	8395	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		CHEMBL1093306	8395	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	599	4	1	3	6.7	CC(=O)NC(C)(C)[C@@H]1CC2(CCN(C(=O)[C@H]3CN(C(C)(C)C)C[C@@H]3c3ccc(F)cc3F)CC2)c2cc(Cl)c(C)cc21	10.1016/j.bmcl.2010.02.058
		44397701	125835	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc4ccccc34)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL364834	125835	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	652	10	2	7	7.0	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCC[C@@H]3c3cccc4ccccc34)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		1338	3807	43	None	53	4	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
		9938402	3807	43	None	53	4	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
		CHEMBL339053	3807	43	None	53	4	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2003.09.036
		44357595	31501	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		CHEMBL140347	31501	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	540	8	2	6	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1)[C@H]1CCCNC1	10.1016/j.bmcl.2003.09.036
		1324	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16154396	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		16197727	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		44285019	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		57514683	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		91898441	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		CHEMBL441738	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		DB04931	302	25	None	-3	4	Human	8.1	pIC50	=	8.1	Binding	Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cellsDisplacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm500064t
		163196518	192129	2	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5203580	192129	2	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		168295644	192312	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		CHEMBL5206336	192312	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assayDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay	ChEMBL	1106	17	13	12	1.5	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSCc2ccccc2CSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c01848
		44349461	16896	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL125079	16896	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	570	9	0	5	4.7	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCSC2)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2003.10.056
		44349227	118473	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	629	11	0	6	3.6	CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL341316	118473	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptorInhibitory activity against [125I]NDP-alpha-MSH binding to the human melanocortin 4 receptor	ChEMBL	629	11	0	6	3.6	CCN1CCN(C(=O)C[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3N(CC3CC3)S(C)(=O)=O)CC2)CC1	10.1016/j.bmcl.2003.10.056
		CHEMBL3349030	211405	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		52947911	18152	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		CHEMBL1269571	18152	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Inhibition of human MC4 receptorInhibition of human MC4 receptor	ChEMBL	623	4	0	4	8.1	Cc1cnc(C(C)(C)[C@H]2CC3(CCN(C(=O)[C@@H]4CN(C(C)(C)C)C[C@H]4c4ccc(F)cc4F)CC3)c3cc(Cl)c(C)cc32)o1	10.1016/j.bmcl.2010.09.049
		44448588	95321	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		CHEMBL256526	95321	0	None	-	0	Human	8.0	pIC50	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cellsDisplacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	ChEMBL	609	6	1	3	7.3	CC[C@H](NC(C)=O)c1cc(Cl)ccc1C1CCN(C(=O)[C@H]2CN(C(C)(C)C)C[C@@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2008.04.049
		127047475	139749	0	None	-	0	Mouse	8.0	pIC50	=	8	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		132991507	139749	0	None	-	0	Mouse	8.0	pIC50	=	8	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		CHEMBL3798421	139749	0	None	-	0	Mouse	8.0	pIC50	=	8	Binding	Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysisDisplacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis	ChEMBL	1630	54	21	19	-1.2	CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCCOCCOCCOCCCNC(=O)COCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/acs.jmedchem.5b01894
		44357575	26888	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	604	11	2	6	4.7	O=C(CCNC(=O)c1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		CHEMBL136366	26888	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Binding activity was measured using membranes of Hi5 cells expressing the human MC4R receptorsBinding activity was measured using membranes of Hi5 cells expressing the human MC4R receptors	ChEMBL	604	11	2	6	4.7	O=C(CCNC(=O)c1ccccc1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2003.09.036
		15602927	157882	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		CHEMBL408398	157882	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from MC4RDisplacement of [125I]NDP-alpha-MSH from MC4R	ChEMBL	835	12	10	8	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC(=O)NCCN(CC(N)=O)C(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm701093y
		44426649	153134	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	737	21	10	7	0.4	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2007.04.001
		CHEMBL397652	153134	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cellsDisplacement of Eu-NDP-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells	ChEMBL	737	21	10	7	0.4	C#CCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmcl.2007.04.001
		44358622	13662	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL1194620	13662	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL553000	13662	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	602	10	2	7	5.9	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNCC[C@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL413260	213059	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm960845e
		CHEMBL65339	215860	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uMDisplacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM	ChEMBL		None	None	None		CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm960840h
		44423471	142524	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	571	11	0	5	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(N(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		CHEMBL389073	142524	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cellsDisplacement of [125I]Nle4-D-Phe7-alpha-MSH from human MC4 receptor expressed in COS1 cells	ChEMBL	571	11	0	5	5.9	CC(C)N1CCN(C(CN2CCN(CCCc3ccccc3-c3ccc(N(C)C)cc3)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2006.12.039
		44310243	169187	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		91932909	169187	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		CHEMBL440633	169187	0	None	-	0	Mouse	5.0	pIC50	=	5.0	Binding	Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSHInhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]NDP-MSH	ChEMBL	1421	24	20	20	-4.6	C[C@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NN)CC(=O)NC(C(=O)NN[C@H](Cc2ccc(O)cc2)C(=O)C(=O)O)NC(=O)C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/jm0303608
		44315095	103133	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	559	13	3	4	4.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		CHEMBL307857	103133	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligandBinding affinity towards human melanocortin 4 receptor (hMC4R) using [125I]NDP-alpha-MSH as radioligand	ChEMBL	559	13	3	4	4.2	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N(CCCCN)C1CCC(N(CCc2c[nH]c3ccccc23)C(C)=O)CC1	10.1016/s0960-894x(03)00412-8
		137639815	156802	0	None	-	1	Mouse	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		CHEMBL4071063	156802	0	None	-	1	Mouse	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma countingDisplacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting	ChEMBL	847	20	11	8	0.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/acs.jmedchem.7b00301
		56676634	63684	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		CHEMBL1801124	63684	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation countingDisplacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	ChEMBL	667	5	1	3	7.5	Cc1cc2c(cc1Cl)C1(CCN(C(=O)[C@@H]3CN(C(C)(C)C)C[C@H]3c3ccc(F)cc3F)CC1)C[C@H]2C(C)(C)C(=O)NCC(F)(F)F	10.1016/j.bmcl.2010.06.062
		44397355	127151	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL365675	127151	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	634	10	1	7	6.4	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)N(C)C(=O)C3CNCCC3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL3349030	211405	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Binding affinity for Human Melanocortin 4 receptor expressed in L-cellsBinding affinity for Human Melanocortin 4 receptor expressed in L-cells	ChEMBL		None	None	None		CSCC[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)O	10.1021/jm000211e
		44445084	160739	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	829	9	11	9	0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		CHEMBL411391	160739	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	829	9	11	9	0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CCCCC(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm070461w
		44390423	63764	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL180157	63764	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	In vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligandIn vitro inhibitory concentration required against melanocortin 4 receptor using [125I]NDP-MSH as radioligand	ChEMBL	645	10	1	6	4.8	CS(=O)(=O)N(CC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2005.01.060
		CHEMBL3601431	211827	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		145948876	167483	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
		CHEMBL4299441	167483	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysisDisplacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis	ChEMBL	1220	17	14	11	1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/acs.jmedchem.5b01285
		44397661	123801	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL362314	123801	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	621	10	2	8	5.1	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNCCN3c3ccc(F)cc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44358848	118984	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL342470	118984	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)Concentration required to inhibit binding of [125I]-NDP-alpha-MSH from membranes prepared from CHO cells expressing human melanocortin subtype-4-receptor (MC4R)	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2003.09.026
		CHEMBL3600912	211821	0	None	-	1	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C1=O	10.1021/acs.jmedchem.5b00102
		44358630	28314	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL137452	28314	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		CHEMBL541866	28314	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cellsInhibition of [125I]-NDP- alpha-MSH binding to human melanocortin 4 receptor expressed in CHO cells	ChEMBL	588	10	2	7	5.5	COc1ccc(-n2nc(Sc3ccc(Cl)cc3)cc(CC[C@@H](C)NC(=O)[C@H]3CNC[C@@H]3c3ccccc3)c2=O)cc1	10.1016/j.bmcl.2005.06.033
		44423380	13085	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL1190224	13085	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL540373	13085	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Displacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cellsDisplacement of [125I][Nle4,D-Phe7]alphaMSH from human MC4R expressed in COS7 cells	ChEMBL	545	10	0	3	7.1	CC(C)N1CCC(C(CN2CCN(CCCc3ccccc3-c3ccccc3F)CC2)c2ccc(F)cc2)CC1	10.1016/j.bmc.2007.01.019
		CHEMBL3600920	211823	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence countingDisplacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC4 receptor expressed in HEK293 cells after 40 mins by luminescence counting	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)N(C)C(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.5b00102
		CHEMBL2371971	210168	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cellsDisplacement of [125I]NDPalphaMSH from human cloned MC4R expressed in CHO cells	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](c2ccccc2)NC1=O	10.1021/jm0614275
		1325	3600	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		6440621	3600	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		9898183	3600	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		CHEMBL3422426	3600	14	None	-1	7	Mouse	10.4	pKd	=	10.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.5b00184
		44366081	10262	0	None	2	2	Human	9.8	pKd	=	9.8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		CHEMBL1161313	10262	0	None	2	2	Human	9.8	pKd	=	9.8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL	1036	15	13	11	0.4	CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		1325	3600	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		6440621	3600	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		9898183	3600	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		CHEMBL3422426	3600	14	None	-1	7	Mouse	9.7	pKd	=	9.7	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		None	10.1021/ml500340z
		CHEMBL440801	213869	0	None	25	2	Human	9.7	pKd	=	9.7	Binding	pA2 against human melanocortin receptor, human Melanocortin 4 receptorpA2 against human melanocortin receptor, human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303103
		CHEMBL2096742	209206	0	None	5	2	Human	9.3	pKd	=	9.3	Binding	pA2 against human melanocortin receptor, human Melanocortin 4 receptorpA2 against human melanocortin receptor, human Melanocortin 4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0303103
		CHEMBL1161322	208508	0	None	1	2	Human	9.3	pKd	=	9.3	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm0202526
		122178167	121260	0	None	162	2	Mouse	9.1	pKd	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577996	121260	0	None	162	2	Mouse	9.1	pKd	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL2096742	209206	0	None	5	2	Human	9.1	pKd	=	9.1	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm0202526
		CHEMBL1161323	208509	0	None	5	2	Human	8.9	pKd	=	8.9	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2C[C@@]3(C)CCCC[C@@]3(C)N2C1=O	10.1021/jm0202526
		CHEMBL1161316	208504	0	None	63	2	Human	8.0	pKd	=	8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O	10.1021/jm0202526
		CHEMBL2372589	210273	0	None	-15	2	Human	8.0	pKd	=	8	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3CN2C1=O	10.1021/jm0202526
		122178155	121251	0	None	-	1	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577985	121251	0	None	-	1	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178158	121253	0	None	10	2	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577987	121253	0	None	10	2	Mouse	7.0	pKd	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3422430	211669	0	None	-	1	Mouse	6.0	pKd	=	6	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O	10.1021/ml500340z
		122178161	121255	0	None	-	1	Mouse	5.9	pKd	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577990	121255	0	None	-	1	Mouse	5.9	pKd	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		118735604	118877	0	None	251	2	Mouse	7.8	pKd	=	7.8	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	860	18	10	6	2.0	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml500340z
		CHEMBL3422427	118877	0	None	251	2	Mouse	7.8	pKd	=	7.8	Binding	Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisCompetitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	860	18	10	6	2.0	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/ml500340z
		122178157	121252	0	None	50	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577986	121252	0	None	50	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178164	121258	0	None	158	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577993	121258	0	None	158	2	Mouse	7.8	pKd	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3422431	211670	0	None	-	1	Mouse	6.8	pKd	=	6.8	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	10.1021/ml500340z
		CHEMBL3577977	211745	0	None	3	2	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577980	211748	0	None	7	2	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577982	211750	0	None	3	2	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577988	211751	0	None	-	1	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3578001	211755	0	None	-	1	Mouse	6.8	pKd	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577981	211749	1	None	29	3	Mouse	7.7	pKd	=	7.7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL1161321	208507	0	None	19	2	Human	7.7	pKd	=	7.7	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(Cc3ccccc3C2)NC1=O	10.1021/jm0202526
		CHEMBL2372588	210272	0	None	316	2	Human	8.6	pKd	=	8.6	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2Cc3ccccc3N2C1=O	10.1021/jm0202526
		122178168	121261	0	None	25	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577997	121261	0	None	25	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577995	211752	0	None	6	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3578000	211754	0	None	50	2	Mouse	8.4	pKd	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL1161318	208505	0	None	79	2	Human	8.4	pKd	=	8.4	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCCC2)NC1=O	10.1021/jm0202526
		CHEMBL3577976	211744	0	None	2	2	Mouse	6.5	pKd	=	6.5	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		CHEMBL1161320	208506	0	None	-12	2	Human	6.5	pKd	=	6.5	Binding	pA2 value for human Melanocortin-4 receptorpA2 value for human Melanocortin-4 receptor	ChEMBL		None	None	None		CCCC[C@@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CC2)NC1=O	10.1021/jm0202526
		118735609	118880	0	None	251	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		CHEMBL3422432	118880	0	None	251	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		118735610	118881	0	None	398	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		CHEMBL3422433	118881	0	None	398	2	Mouse	8.3	pKd	=	8.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	871	18	9	6	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(N)=O	10.1021/ml500340z
		122178169	121262	0	None	31	2	Mouse	8.3	pKd	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577998	121262	0	None	31	2	Mouse	8.3	pKd	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577999	211753	0	None	19	2	Mouse	8.3	pKd	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		118735605	118878	0	None	-	1	Mouse	6.3	pKd	=	6.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	897	19	9	6	3.2	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/ml500340z
		CHEMBL3422428	118878	0	None	-	1	Mouse	6.3	pKd	=	6.3	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	897	19	9	6	3.2	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(-c2ccccc2)cc1)C(N)=O	10.1021/ml500340z
		122178162	121256	0	None	-	1	Mouse	8.2	pKd	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577991	121256	0	None	-	1	Mouse	8.2	pKd	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178165	121259	0	None	-	1	Mouse	7.2	pKd	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577994	121259	0	None	-	1	Mouse	7.2	pKd	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577978	211746	0	None	10	2	Mouse	7.2	pKd	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		118735606	118879	0	None	-	1	Mouse	7.1	pKd	=	7.1	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	877	18	9	7	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/ml500340z
		CHEMBL3422429	118879	0	None	-	1	Mouse	7.1	pKd	=	7.1	Binding	Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysisAntagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis	ChEMBL	877	18	9	7	2.7	CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1csc2ccccc12)C(N)=O	10.1021/ml500340z
		162676295	183453	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4798971	183453	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162676295	183453	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4798971	183453	0	None	2	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(F)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673931	183058	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794168	183058	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673931	183058	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794168	183058	0	None	8	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cn(nn2)CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673650	183053	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794121	183053	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162673650	183053	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794121	183053	0	None	1	2	Human	10.8	pKi	=	10.8	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(Cl)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643092	181724	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4777048	181724	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643092	181724	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4777048	181724	0	None	1	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3cc(Cl)ccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672837	183021	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4793821	183021	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162668987	182590	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4788071	182590	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672837	183021	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4793821	183021	0	None	18	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1098	17	13	13	0.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1Cc2cnnn2CCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162668987	182590	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4788071	182590	0	None	15	2	Human	10.7	pKi	=	10.7	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3c(F)cccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672763	183124	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794990	183124	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672763	183124	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4794990	183124	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1092	17	14	11	0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672255	182871	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791788	182871	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162672255	182871	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791788	182871	0	None	13	2	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		1325	3600	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		6440621	3600	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		9898183	3600	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL3422426	3600	14	None	1	7	Human	10.6	pKi	=	10.6	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		1325	3600	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		6440621	3600	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		9898183	3600	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL3422426	3600	14	None	1	7	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		162677133	183557	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4800268	183557	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162677133	183557	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4800268	183557	0	None	19	2	Human	10.5	pKi	=	10.5	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1108	17	14	11	0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccc(Cl)cc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643518	181711	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776915	181711	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162643518	181711	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776915	181711	0	None	89	2	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1075	17	15	12	-1.3	CC(=O)N[C@H](CCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		166585475	191540	0	None	-	1	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	475	5	1	7	3.9	COc1cc(OC)cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5cnn(C)c5)c(C)nc4N3)C2)c1	10.1021/acsmedchemlett.2c00229
		CHEMBL5194472	191540	0	None	-	1	Human	10.4	pKi	=	10.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	475	5	1	7	3.9	COc1cc(OC)cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5cnn(C)c5)c(C)nc4N3)C2)c1	10.1021/acsmedchemlett.2c00229
		1338	3807	43	None	53	4	Human	10.3	pKi	=	10.3	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		9938402	3807	43	None	53	4	Human	10.3	pKi	=	10.3	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL339053	3807	43	None	53	4	Human	10.3	pKi	=	10.3	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL3663320	212052	0	None	9	2	Human	10.3	pKi	=	10.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663321	212053	0	None	3	2	Human	10.3	pKi	=	10.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL442504	213916	0	None	1	3	Human	10.2	pKi	=	10.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm010165y
		CHEMBL3663336	212066	0	None	-	1	Human	10.2	pKi	=	10.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C(F)(F)F)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663319	212051	0	None	3	2	Human	10.1	pKi	=	10.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		57817763	76927	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70690940	76927	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929808	76927	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070251	76927	0	None	38	4	Human	10.1	pKi	=	10.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1988	59	26	26	-3.2	CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL3663337	212067	0	None	-	1	Human	10.1	pKi	=	10.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2C)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL415165	213176	0	None	1	5	Rat	10.1	pKi	=	10.1	Binding	Binding affinity for rat melanocortin-4 receptorBinding affinity for rat melanocortin-4 receptor	ChEMBL		None	None	None		None	10.1021/jm0501432
		89703076	144190	0	None	-4	2	Human	10.0	pKi	=	10.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3904232	144190	0	None	-4	2	Human	10.0	pKi	=	10.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL385465	212351	0	None	10	3	Human	10.0	pKi	=	10.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm010165y
		57646437	76922	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684621	76922	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929804	76922	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070246	76922	0	None	10	4	Human	10.0	pKi	=	10.0	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1855	51	23	23	-2.2	CCCCCCCCCCCCCCCC(=O)NS(=O)(=O)CCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		57646441	76920	0	None	13	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070243	76920	0	None	13	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1706	46	22	20	-1.4	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		59149264	76802	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684624	76802	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929810	76802	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2069317	76802	0	None	22	4	Human	9.9	pKi	=	9.9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1946	57	23	26	-3.0	CCCC[C@H](NC(=O)[C@H](CN(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2415082	210433	0	None	-	1	Human	9.9	pKi	=	9.9	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		CHEMBL415661	213198	0	None	21	4	Human	9.9	pKi	=	9.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		122194229	123983	0	None	-	1	Human	9.9	pKi	=	9.9	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		CHEMBL3629347	123983	0	None	-	1	Human	9.9	pKi	=	9.9	Binding	Inhibition of human recombinant melanocortin 4 receptor expressed in CHO cellsInhibition of human recombinant melanocortin 4 receptor expressed in CHO cells	ChEMBL	1646	50	23	21	-4.1	CCCCC(NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/acs.jmedchem.6b01422
		CHEMBL3663331	212063	0	None	5	2	Human	9.8	pKi	=	9.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		57817773	76925	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684623	76925	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929806	76925	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070249	76925	0	None	58	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@H](CN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		59149266	76926	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70693081	76926	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929807	76926	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070250	76926	0	None	234	4	Human	9.8	pKi	=	9.8	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1918	56	24	26	-3.6	CCCC[C@H](NC(=O)[C@@H](N)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		57817730	76923	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70684622	76923	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929805	76923	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070247	76923	0	None	75	4	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1919	56	24	26	-3.5	CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		166585425	190633	0	None	-	1	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5181223	190633	0	None	-	1	Human	9.7	pKi	=	9.7	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL2370968	209971	0	None	-1	3	Human	9.7	pKi	=	9.7	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		CHEMBL3663327	212059	0	None	1	2	Human	9.6	pKi	=	9.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663332	212064	0	None	-1	2	Human	9.6	pKi	=	9.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		COc1ccc(C[C@H]2NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC2=O)cc1	nan
		CHEMBL3663370	212099	0	None	2	2	Human	9.6	pKi	=	9.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		10408	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		5329	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		9941379	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		CHEMBL2070241	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		DB11653	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/jm201489a
		166585537	190503	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	478	4	1	7	4.0	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5179337	190503	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	478	4	1	7	4.0	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		44347220	168440	0	None	112	3	Human	9.6	pKi	=	9.6	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	861	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL434985	168440	0	None	112	3	Human	9.6	pKi	=	9.6	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	861	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		59149255	76928	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		70693082	76928	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929809	76928	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070252	76928	0	None	13	4	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1960	58	24	26	-2.5	CCCC[C@H](NC(=O)[C@H](CNC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL414718	213151	0	None	-3	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
		CHEMBL331259	211361	0	None	70	3	Human	9.6	pKi	=	9.6	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O	10.1021/jm010165y
		166585598	190143	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	517	4	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc6ccccn6n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5173560	190143	0	None	-	1	Human	9.6	pKi	=	9.6	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	517	4	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc6ccccn6n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL407809	212685	0	None	35	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL3663342	212072	0	None	-	1	Human	9.5	pKi	=	9.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663363	212093	0	None	83	2	Human	9.5	pKi	=	9.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		1324	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		16154396	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		16197727	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		44285019	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		57514683	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		91898441	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		CHEMBL441738	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		DB04931	302	25	None	-3	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		None	10.1021/jm201489a
		CHEMBL412523	213000	0	None	22	4	Human	9.5	pKi	=	9.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL415165	213176	0	None	-3	5	Human	9.5	pKi	=	9.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0501432
		70688853	76924	0	None	9	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070248	76924	0	None	9	4	Human	9.5	pKi	=	9.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1495	39	18	16	-0.1	CCCCCCCCCCCCCCCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL3663378	212107	0	None	34	2	Human	9.5	pKi	=	9.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H]([C@@H](C)OCc2ccccc2)NC1=O	nan
		44347119	114423	0	None	151	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	752	9	10	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL333178	114423	0	None	151	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	752	9	10	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		57646411	76921	0	None	1	4	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070245	76921	0	None	1	4	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1739	49	24	20	-1.7	CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL267900	210737	0	None	1	4	Rat	9.4	pKi	=	9.4	Binding	Binding affinity for rat melanocortin-4 receptorBinding affinity for rat melanocortin-4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		44415919	141588	0	None	2	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL385000	141588	0	None	2	3	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	780	16	6	7	1.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		88590706	125526	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646867	125526	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646851	211996	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590706	125526	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646867	125526	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	19	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)C1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646851	211996	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88287852	127559	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1044	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663335	127559	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1044	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CCN)NC1=O	nan
		166585402	189944	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	531	5	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc(C(F)F)n(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5170290	189944	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	531	5	1	8	4.3	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nc(C(F)F)n(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		1324	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16154396	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		16197727	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		44285019	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		57514683	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		91898441	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		CHEMBL441738	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		DB04931	302	25	None	-3	4	Human	9.4	pKi	=	9.4	Binding	Binding affinity to human MC4 receptor by radioligand displacement assayBinding affinity to human MC4 receptor by radioligand displacement assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2013.01.044
		166585467	190231	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	480	5	1	7	4.0	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)[C@@H](C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5174952	190231	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	480	5	1	7	4.0	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)[C@@H](C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL408257	212704	0	None	23	3	Human	9.4	pKi	=	9.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL3663340	212070	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)[C@H](CCN)NC1=O	nan
		1323	2688	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		92432	2688	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL430239	2688	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		1323	2688	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		92432	2688	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		CHEMBL430239	2688	55	None	-10	3	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.0c01620
		162670951	182838	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791306	182838	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162670951	182838	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4791306	182838	0	None	33	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1100	18	14	11	0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccccc3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		164889476	190794	4	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	462	4	1	7	3.5	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5183637	190794	4	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	462	4	1	7	3.5	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5ncccn5)c(C)nc4N3)C2)c(F)cn1	10.1021/acsmedchemlett.2c00229
		1324	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16154396	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		16197727	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		44285019	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		57514683	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		91898441	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		CHEMBL441738	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		DB04931	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of radiolabeled NDPalpha-MSH from human MC4 receptorDisplacement of radiolabeled NDPalpha-MSH from human MC4 receptor	ChEMBL		None	None	None		None	10.1021/jm8007618
		44347219	16580	0	None	301	3	Human	9.3	pKi	=	9.3	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	781	9	10	8	0.2	NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		CHEMBL123938	16580	0	None	301	3	Human	9.3	pKi	=	9.3	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	781	9	10	8	0.2	NNC(=O)[C@H]1CCCCNC(=O)CCC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		CHEMBL3663334	212065	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663345	212075	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3667945	212139	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		44443035	154417	0	None	-26	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL398929	154417	0	None	-26	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL264352	210617	0	None	1	4	Rat	9.3	pKi	=	9.3	Binding	Binding affinity for rat melanocortin-4 receptorBinding affinity for rat melanocortin-4 receptor	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		CHEMBL2373515	210379	0	None	1	3	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		166585443	190277	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		CHEMBL5175663	190277	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		168288063	191637	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	514	5	1	7	4.6	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3cc(OC(F)F)ncc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5195837	191637	0	None	-	1	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	514	5	1	7	4.6	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3cc(OC(F)F)ncc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		162672691	183201	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4795842	183201	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL266879	210706	0	None	-2	4	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(N)=O	10.1021/jm0501432
		CHEMBL267900	210737	0	None	-1	4	Human	9.3	pKi	=	9.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		162672691	183201	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4795842	183201	0	None	57	2	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3cccc4ccccc34)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		1324	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.3	pKi	=	9.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL408843	212735	0	None	-1	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@@H](C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm010165y
		1324	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44347331	16327	0	None	181	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		CHEMBL122773	16327	0	None	181	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		44410040	76518	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL205996	76518	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	2	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL2070374	209187	0	None	22	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CNC(=O)CN(CC(=O)O)CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		24740655	89086	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
		CHEMBL236521	89086	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1016/j.bmcl.2007.07.097
		44415914	139270	0	None	1	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL379054	139270	0	None	1	3	Human	9.2	pKi	=	9.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	762	16	6	7	1.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44443035	154417	0	None	26	4	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL398929	154417	0	None	26	4	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL3644324	211964	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644324	211964	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663329	212061	0	None	5	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663367	212096	0	None	5	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663368	212097	0	None	10	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		23635109	91559	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635109	91559	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL240572	91559	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL240572	91559	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	540	10	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		24740655	89086	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		CHEMBL236521	89086	0	None	891	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	1	5	5.3	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		1324	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		1324	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		1324	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL3663372	212101	0	None	1	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663343	212073	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644293	211937	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3644348	211987	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		134143749	150612	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1133	19	15	12	3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3955282	150612	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1133	19	15	12	3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3644348	211987	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3663325	212057	0	None	1	2	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663339	212069	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc([N+](=O)[O-])c2)NC(=O)[C@H](CCN)NC1=O	nan
		44433290	96461	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	10	2	5	4.7	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)[C@@H](C)N)c1	10.1016/j.bmcl.2007.07.097
		CHEMBL262321	96461	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	10	2	5	4.7	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@H](CC(C)C)NC(=O)[C@@H](C)N)c1	10.1016/j.bmcl.2007.07.097
		24180646	148182	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393576	148182	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24180646	148182	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL393576	148182	0	None	1	8	Mouse	9.2	pKi	=	9.2	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL267492	210724	0	None	-	1	Human	9.2	pKi	=	9.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		CHEMBL3663318	212050	0	None	1	2	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3667943	212137	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667944	212138	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88944291	153350	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3978439	153350	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL1923665	209087	0	None	1	3	Human	9.1	pKi	=	9.1	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm201226w
		162643435	181667	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776340	181667	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL1923667	209088	0	None	-1	3	Human	9.1	pKi	=	9.1	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm201226w
		CHEMBL264352	210617	0	None	-1	4	Human	9.1	pKi	=	9.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		162643435	181667	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4776340	181667	0	None	4	2	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3cccc4ccccc34)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		122178167	121260	0	None	162	2	Mouse	9.1	pKi	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577996	121260	0	None	162	2	Mouse	9.1	pKi	=	9.1	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	948	11	10	10	-1.1	C[C@@H]1NC(=O)C(CN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44415913	79951	0	None	-1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL212614	79951	0	None	-1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	16	6	7	0.8	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		88590696	125527	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646868	125527	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590696	125527	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646868	125527	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.0	N=C(N)NCCC[C@H](NC(=O)CC1CCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		44434550	88529	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	641	9	3	5	5.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCNCC2)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL235190	88529	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	641	9	3	5	5.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCNCC2)CC1	10.1016/j.bmc.2007.05.026
		44434562	88698	0	None	301	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236014	88698	0	None	301	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		44577093	178646	0	None	42	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL467587	178646	0	None	42	3	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	9	2	5	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)[C@@H](C)N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		1324	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		10325306	141264	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL383117	141264	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	550	12	2	4	5.5	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL3663323	212055	0	None	6	2	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL268851	210769	0	None	33	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@@H]1CC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		44347221	16635	0	None	53	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL124169	16635	0	None	53	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44432941	87563	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233559	87563	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		24180593	148443	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393788	148443	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	5.0	CC(C)C[C@H](NCCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL3667940	212134	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44432941	87563	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233559	87563	0	None	-	1	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	575	14	1	7	7.0	COC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		24180646	148182	0	None	-1	8	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL393576	148182	0	None	-1	8	Human	9.1	pKi	=	9.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		168277761	190300	0	None	-1	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2342	37	34	29	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5175981	190300	0	None	-1	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2342	37	34	29	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		162665450	182296	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4784053	182296	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		162665450	182296	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4784053	182296	0	None	10	2	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(-c3ccc4ccccc4c3)c2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL267492	210724	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		24180646	148182	0	None	-1	8	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393576	148182	0	None	-1	8	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433276	89675	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.9	CC(C)C[C@H](NCCCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237578	89675	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.9	CC(C)C[C@H](NCCCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		1324	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		16154396	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		16197727	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		44285019	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		57514683	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		91898441	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		CHEMBL441738	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		DB04931	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		None	10.1016/s0960-894x(03)00552-3
		CHEMBL3663330	212062	0	None	9	2	Human	9.0	pKi	=	9.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C(F)(F)F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663369	212098	0	None	-1	2	Human	9.0	pKi	=	9.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44432966	146301	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL392092	146301	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432966	146301	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL392092	146301	0	None	562	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	0	6	6.7	COc1ccc(C(=O)c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		1324	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44433270	89083	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	641	11	2	5	5.5	CC(C)C[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236519	89083	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	641	11	2	5	5.5	CC(C)C[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433287	161266	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	11	2	5	4.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL412023	161266	0	None	-	1	Human	9.0	pKi	=	9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	11	2	5	4.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24180646	148182	0	None	-1	8	Rat	9.0	pKi	=	9	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393576	148182	0	None	-1	8	Rat	9.0	pKi	=	9	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		10257541	126342	0	None	123	4	Human	9.0	pKi	=	9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL365039	126342	0	None	123	4	Human	9.0	pKi	=	9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		88212540	125066	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644356	125066	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		89007953	151630	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3963781	151630	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644316	211956	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646856	212000	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590676	125528	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646869	125528	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644292	211936	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)OCc2ccccc2)NC1=O	nan
		88212540	125066	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644356	125066	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1107	19	17	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590676	125528	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646869	125528	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1112	20	17	12	-1.6	N=C(N)NCCC[C@H](NC(=O)CC1CCCCC1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134153366	152795	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1121	20	16	12	3.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)OCc2ccccc2)/N=C\1O	nan
		CHEMBL3973691	152795	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1121	20	16	12	3.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)OCc2ccccc2)/N=C\1O	nan
		90684343	160183	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1069	18	17	11	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL4109346	160183	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1069	18	17	11	-3.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL3644316	211956	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646856	212000	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663349	212079	0	None	144	2	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3663366	212095	0	None	1	2	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3663375	212104	0	None	89	2	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3667939	212133	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667947	212141	0	None	-	1	Human	9.0	pKi	=	9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL2070244	209184	0	None	4	4	Human	9.0	pKi	=	9	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44434548	148350	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL393716	148350	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		44456222	97925	0	None	223	3	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272538	97925	0	None	223	3	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44456102	155604	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL404549	155604	0	None	-	1	Human	9.0	pKi	=	9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL2370154	209801	0	None	1	3	Human	9.0	pKi	=	9	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm020021z
		44433296	153045	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	669	11	2	5	5.4	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397581	153045	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	669	11	2	5	5.4	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416057	81191	0	None	1	3	Human	9.0	pKi	=	9.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL215833	81191	0	None	1	3	Human	9.0	pKi	=	9.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	745	17	6	7	0.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44577092	178645	0	None	11	3	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL467586	178645	0	None	11	3	Human	9.0	pKi	=	9.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	548	10	2	5	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		25022598	95030	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL255007	95030	0	None	-	1	Human	9.0	pKi	=	9.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		1324	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		11017471	31917	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm049278i
		CHEMBL140738	31917	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	603	8	2	7	4.0	Cn1nnc(CC2(C3CCCCC3)CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)n1	10.1021/jm049278i
		CHEMBL412495	212998	0	None	12	3	Human	8.9	pKi	=	8.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		1323	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
		92432	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
		CHEMBL430239	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.8b00170
		1323	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		92432	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		CHEMBL430239	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		1323	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		92432	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		CHEMBL430239	2688	55	None	-10	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		44400814	70621	0	None	446	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	627	11	3	5	5.9	O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL194990	70621	0	None	446	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	627	11	3	5	5.9	O=C(NC1CCCC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44415920	80371	0	None	3	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL214410	80371	0	None	3	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	644	12	4	6	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)N2CCNCC2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44416106	141446	0	None	5	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL384176	141446	0	None	5	3	Human	8.9	pKi	=	8.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	617	12	4	5	1.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44577095	178754	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	9	2	5	4.6	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL468636	178754	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	9	2	5	4.6	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL267492	210724	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		1324	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		162669632	182565	0	None	6	2	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		CHEMBL4787753	182565	0	None	6	2	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 minsDisplacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins	ChEMBL	1150	18	14	11	1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(-c3ccc4ccccc4c3)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	10.1021/acs.jmedchem.0c01620
		44433298	153047	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397583	153047	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	2	5	5.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433277	168926	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	655	12	2	5	5.9	CC(C)C[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL438683	168926	0	None	-	1	Human	8.9	pKi	=	8.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	655	12	2	5	5.9	CC(C)C[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400810	124060	0	None	316	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	11	3	5	5.4	CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL363190	124060	0	None	316	2	Human	8.9	pKi	=	8.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	11	3	5	5.4	CC(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44456222	97925	0	None	223	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272538	97925	0	None	223	3	Human	8.9	pKi	=	8.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		25131478	169508	0	None	44	3	Human	8.9	pKi	=	8.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
		CHEMBL443396	169508	0	None	44	3	Human	8.9	pKi	=	8.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	574	10	5	6	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C/C=N/NC(=N)N)C1=O	10.1021/jm800525p
		CHEMBL2370963	209966	0	None	10	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44347331	16327	0	None	181	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		CHEMBL122773	16327	0	None	181	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	794	10	9	7	1.3	CCC1CC(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](C(N)=O)CCCCNC1=O	10.1021/jm010165y
		CHEMBL2370553	209870	0	None	10	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm010165y
		44433271	89539	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
		CHEMBL237365	89539	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	1	5	5.0	CC(C)C[C@@H](c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1)N(C)CCN	10.1016/j.bmcl.2007.07.097
		44433299	153048	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397584	153048	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	629	12	1	5	5.0	CC(C)C[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400935	70862	0	None	104	4	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	10	2	5	5.5	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195110	70862	0	None	104	4	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	10	2	5	5.5	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)N1CCCC1	10.1016/j.bmcl.2005.03.053
		CHEMBL2415084	210435	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(N)=O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		CHEMBL267492	210724	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		CHEMBL420167	213242	0	None	8	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		44412933	76623	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	611	13	3	6	4.1	COc1ccccc1CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL206364	76623	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	611	13	3	6	4.1	COc1ccccc1CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44400864	124325	0	None	177	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	11	3	5	5.0	CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL363576	124325	0	None	177	3	Human	8.8	pKi	=	8.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	11	3	5	5.0	CCNC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562476	186015	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL487044	186015	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL2415081	210432	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		56851058	69073	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		57394091	69073	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		91930626	69073	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		CHEMBL1923666	69073	0	None	-1	3	Human	8.8	pKi	=	8.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1823	57	25	20	-0.9	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		CHEMBL267492	210724	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432950	86791	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232162	86791	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432950	86791	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232162	86791	0	None	-	1	Human	8.8	pKi	=	8.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	621	15	1	6	8.4	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(=O)c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		6918814	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL365597	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		6918814	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL365597	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL2415019	210430	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCCc1cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44434546	88799	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236423	88799	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		44434547	88800	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236424	88800	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		6918814	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL365597	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		6918814	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL365597	127057	1	None	58	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	587	12	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44443033	93698	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL247010	93698	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(F)c1	10.1016/j.bmcl.2007.10.032
		44433294	153043	0	None	575	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397580	153043	0	None	575	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		10077773	87267	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233135	87267	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44409103	140123	0	None	-1	3	Human	8.0	pKi	=	8	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
		CHEMBL380120	140123	0	None	-1	3	Human	8.0	pKi	=	8	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	628	15	5	6	2.4	CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccccc2)C[C@@H]1CCCN=C(N)N	10.1016/j.bmcl.2005.12.005
		44391382	130454	0	None	-	1	Human	8.0	pKi	=	8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	9	4	6	4.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL368023	130454	0	None	-	1	Human	8.0	pKi	=	8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	9	4	6	4.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3663351	212081	0	None	81	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3663361	212091	0	None	1000	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3667925	212119	0	None	39	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667928	212122	0	None	21	2	Human	8.0	pKi	=	8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44434549	89166	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236625	89166	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		16038316	79756	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	583	11	2	6	4.1	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211742	79756	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	583	11	2	6	4.1	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		44444509	93968	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL248435	93968	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	663	11	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447250	94727	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL253028	94727	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		44577090	178666	0	None	57	3	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL467771	178666	0	None	57	3	Human	8.0	pKi	=	8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	9	2	4	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		46885482	8330	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092860	8330	0	None	-	1	Human	8.0	pKi	=	8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		11845272	80358	0	None	4	3	Human	8.0	pKi	=	8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL214347	80358	0	None	4	3	Human	8.0	pKi	=	8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		44412510	138401	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	635	11	2	6	4.6	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CN2CCOCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL377313	138401	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	635	11	2	6	4.6	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CN2CCOCC2)CC1	10.1016/j.bmcl.2006.04.002
		44412613	138926	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL378411	138926	0	None	-	1	Human	8.0	pKi	=	8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL5090670	215277	0	None	1	3	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](C)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44410803	140172	0	None	87	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380365	140172	0	None	87	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL5090285	215253	0	None	-3	3	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		11181804	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		CHEMBL366706	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		44323034	206530	0	None	-2	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL88537	206530	0	None	-2	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	729	21	11	8	-0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44323032	206604	0	None	-5	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL89004	206604	0	None	-5	3	Human	7.0	pKi	=	7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	761	20	10	7	0.8	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL3644311	211951	0	None	-	1	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644311	211951	0	None	-	1	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88944278	149540	0	None	-6606	2	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	967	19	13	10	-0.2	CCCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3946641	149540	0	None	-6606	2	Human	7.0	pKi	=	7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	967	19	13	10	-0.2	CCCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		122178155	121251	0	None	-	1	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577985	121251	0	None	-	1	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178158	121253	0	None	10	2	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577987	121253	0	None	10	2	Mouse	7.0	pKi	=	7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44433409	152214	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	9	1	4	6.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL396868	152214	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	9	1	4	6.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44405450	72518	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL199061	72518	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	11	2	5	3.1	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44405364	72522	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	10	2	5	4.5	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccco3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL199073	72522	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	10	2	5	4.5	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccco3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447224	154700	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	9	2	6	4.6	CN[C@H](C)C(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL399762	154700	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	9	2	6	4.6	CN[C@H](C)C(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44442992	93923	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	1	5	5.0	COCC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248206	93923	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	1	5	5.0	COCC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443004	94488	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.7	CNCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251495	94488	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.7	CNCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404576	71952	0	None	-	1	Human	7.0	pKi	=	7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1ccc(F)cc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL197288	71952	0	None	-	1	Human	7.0	pKi	=	7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1ccc(F)cc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44413684	11818	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	635	10	2	5	4.8	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(=O)C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182072	11818	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	635	10	2	5	4.8	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(=O)C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL209417	11818	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	635	10	2	5	4.8	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(=O)C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		44393418	155700	0	None	3	4	Human	6.0	pKi	=	6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL405150	155700	0	None	3	4	Human	6.0	pKi	=	6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44395572	66440	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	467	9	1	4	5.0	O=C(CCc1ccc(Cl)cc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL185200	66440	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	467	9	1	4	5.0	O=C(CCc1ccc(Cl)cc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44395464	66976	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccccc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186794	66976	0	None	-	1	Human	6.0	pKi	=	6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccccc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44405563	72450	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	12	2	4	5.0	CCC(CC)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198837	72450	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	12	2	4	5.0	CCC(CC)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44412680	78831	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211280	78831	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		44412690	79452	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	4	6	3.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211366	79452	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	4	6	3.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44415430	79963	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	9	1	4	5.6	NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212653	79963	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	9	1	4	5.6	NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44432885	86997	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232388	86997	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		70685981	75074	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	351	7	3	3	1.5	O=C(NCCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035936	75074	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	351	7	3	3	1.5	O=C(NCCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		70683848	75085	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	540	12	2	5	3.4	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCOc2ccccc2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035947	75085	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	540	12	2	5	3.4	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCOc2ccccc2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL263878	210598	0	None	-45	3	Human	5.0	pKi	=	5	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		88944295	142975	0	None	-1122	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	910	15	11	10	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3894392	142975	0	None	-1122	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	910	15	11	10	-1.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660698	143273	0	None	-288	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3896855	143273	0	None	-288	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		70660688	143698	0	None	-4	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	783	13	10	9	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3900322	143698	0	None	-4	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	783	13	10	9	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		68342929	147614	0	None	-32	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	825	13	12	9	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3931237	147614	0	None	-32	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	825	13	12	9	-1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		88944294	147931	0	None	-12589	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	15	11	10	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3933740	147931	0	None	-12589	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	15	11	10	-0.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660676	148380	0	None	-562	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3937437	148380	0	None	-562	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCCN)NC1=O	nan
		70660680	149054	0	None	-251	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	836	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3942841	149054	0	None	-251	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	836	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		70660654	150154	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	830	17	12	11	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3951584	150154	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	830	17	12	11	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		70660696	150738	0	None	-1	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	667	11	8	8	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3956317	150738	0	None	-1	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	667	11	8	8	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660690	151490	0	None	-331	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3962394	151490	0	None	-331	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCCN)NC1=O	nan
		70660691	151590	0	None	-3311	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	814	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3963435	151590	0	None	-3311	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	814	16	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		88878681	151716	0	None	-6760	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3964400	151716	0	None	-6760	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660651	151886	0	None	-15	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	738	11	9	9	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3965807	151886	0	None	-15	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	738	11	9	9	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660679	153019	0	None	-501	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3975629	153019	0	None	-501	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	818	16	12	10	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		88878668	154285	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3986527	154285	0	None	-5011	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		70660695	154310	0	None	-1412	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	823	15	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3986675	154310	0	None	-1412	2	Human	5.0	pKi	=	5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	823	15	12	10	-2.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44434621	146305	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	561	9	1	5	6.4	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL392094	146305	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	561	9	1	5	6.4	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C13CC4CC(CC(C4)C1)C3)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		44434581	167051	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	7	2	2	5.2	NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL428903	167051	0	None	-3	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	7	2	2	5.2	NCCN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		11845440	138672	0	None	-8	3	Human	6.0	pKi	=	6.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
		CHEMBL377778	138672	0	None	-8	3	Human	6.0	pKi	=	6.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.7	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCNCC1	10.1021/jm060384p
		44393877	122253	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL359777	122253	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	10	4	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCC2CCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		168283887	191020	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186784	191020	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		11851038	140335	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44409240	74434	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
		CHEMBL202699	74434	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2005.12.005
		44409240	74434	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		CHEMBL202699	74434	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		44409240	74434	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
		CHEMBL202699	74434	0	None	16	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	736	18	8	7	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O	10.1021/jm060384p
		44432885	86997	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232388	86997	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	15	2	8	5.2	CCCCN(CCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		44401386	69524	0	None	2	2	Human	6.0	pKi	=	6.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	593	12	6	4	3.6	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL193409	69524	0	None	2	2	Human	6.0	pKi	=	6.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	593	12	6	4	3.6	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)Nc1ccccc1	10.1016/j.bmcl.2005.03.120
		44404544	72120	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(C)=O	10.1016/j.bmcl.2005.08.018
		CHEMBL197820	72120	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(C)=O	10.1016/j.bmcl.2005.08.018
		46203215	8470	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1093856	8470	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1204065	8470	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	428	3	1	3	3.6	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		10304794	139405	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	139405	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44401587	10301	0	None	-1	2	Human	5.0	pKi	=	5.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	611	15	6	5	2.6	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL1161794	10301	0	None	-1	2	Human	5.0	pKi	=	5.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	611	15	6	5	2.6	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1CN)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44401367	161719	0	None	-1	2	Human	7.0	pKi	=	7.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL413565	161719	0	None	-1	2	Human	7.0	pKi	=	7.0	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)cc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		168293053	192066	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5202611	192066	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44432927	87400	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL233357	87400	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL3667954	212148	0	None	9	2	Human	6.0	pKi	=	6.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(=O)O)NC1=O	nan
		10481883	77335	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL208376	77335	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	522	12	2	5	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1ccsc1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		11181804	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		CHEMBL366706	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		44562558	174153	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCCC(C)(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454663	174153	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCCC(C)(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44562559	188960	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508285	188960	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44416135	80184	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL213566	80184	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1016/j.bmcl.2006.05.087
		11181804	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL366706	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL3663338	212068	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2[N+](=O)[O-])NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663348	212078	0	None	48	2	Human	8.0	pKi	=	8.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		CHEMBL3663371	212100	0	None	2	2	Human	8.0	pKi	=	8.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC1=O	nan
		CHEMBL2331674	209532	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)(NC(=O)CNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(=O)NCCC(N)=O)nn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		44393887	66674	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185417	66674	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	613	9	3	5	5.0	CC(NC1CCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		11181804	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL366706	128507	0	None	21	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		23661656	169044	0	None	-1	5	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL439560	169044	0	None	-1	5	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		24873537	146061	0	None	20	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL391902	146061	0	None	20	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44405360	133561	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL371063	133561	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44444497	155012	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		CHEMBL401465	155012	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.3	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		44447785	95077	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255313	95077	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44447777	155415	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403675	155415	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442965	149659	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
		CHEMBL394744	149659	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	520	8	1	6	3.8	Cc1c(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccccc4)CC3)CCCCC2)cnn1C	10.1016/j.bmcl.2007.10.032
		44443031	154556	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL399112	154556	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	8	1	4	5.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44416135	80184	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
		CHEMBL213566	80184	0	None	42	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	561	10	5	5	1.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(=N)N)C1=O	10.1021/jm800525p
		25133208	171994	0	None	13	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
		CHEMBL447117	171994	0	None	13	3	Human	8.0	pKi	=	8.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.1	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCC1	10.1021/jm800525p
		44397281	126544	0	None	109	3	Human	8.0	pKi	=	8.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	12	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365237	126544	0	None	109	3	Human	8.0	pKi	=	8.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	12	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44432903	87193	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232724	87193	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44347105	113346	0	None	13	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	724	9	10	7	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL331728	113346	0	None	13	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	724	9	10	7	-0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC(C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44410378	76626	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
		CHEMBL206367	76626	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	538	11	2	3	5.6	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1Cl	10.1016/j.bmcl.2006.01.016
		44562368	175747	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	8	2	5	4.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)N2CCCC2=O)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL458329	175747	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	8	2	5	4.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)N2CCCC2=O)CC1	10.1016/j.bmcl.2008.07.076
		44562424	179214	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	2	5	4.3	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL472553	179214	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	2	5	4.3	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44562498	186733	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488719	186733	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44562361	188679	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	643	12	0	6	7.0	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL503909	188679	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	643	12	0	6	7.0	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		44322923	206546	0	None	-1	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL88630	206546	0	None	-1	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	710	19	10	8	-0.5	N#CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391289	65566	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	700	12	3	8	3.8	CCOC(=O)C1CCN(CNCc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183114	65566	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	700	12	3	8	3.8	CCOC(=O)C1CCN(CNCc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		44391262	128508	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	645	14	3	6	4.6	CC(C)COCCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL366708	128508	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	645	14	3	6	4.6	CC(C)COCCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44396114	124351	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	3	6	4.0	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL363688	124351	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	3	6	4.0	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		10325955	165271	0	None	6	4	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL423101	165271	0	None	6	4	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	582	8	2	6	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		117723618	150838	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1087	20	18	13	-4.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCNC(=O)CN)NC1=O	nan
		CHEMBL3957057	150838	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1087	20	18	13	-4.5	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCNC(=O)CN)NC1=O	nan
		CHEMBL3644342	211982	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCNC(=O)CN)NC1=O	nan
		88944178	146481	0	None	-4365	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	953	18	13	10	-0.5	CCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3922330	146481	0	None	-4365	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	953	18	13	10	-0.5	CCCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88878681	151716	0	None	-6760	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3964400	151716	0	None	-6760	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44433389	154711	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.2	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL399802	154711	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.2	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44415674	80121	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213264	80121	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415417	80146	0	None	10	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213380	80146	0	None	10	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405613	134224	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	9	2	4	3.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL371683	134224	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	9	2	4	3.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44447236	154806	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.9	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2CC(=O)OC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400274	154806	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.9	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2CC(=O)OC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44432927	87400	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL233357	87400	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccccc1Nc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		44447770	95662	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL258035	95662	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	458	5	2	4	3.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44447776	161891	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL415094	161891	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44443036	93887	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	9	0	5	5.8	COc1ccc(CN(C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL248048	93887	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	9	0	5	5.8	COc1ccc(CN(C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44443018	154309	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	620	9	1	5	6.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4OC(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398667	154309	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	620	9	1	5	6.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4OC(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443006	155166	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.9	NCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL402266	155166	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	2	5	3.9	NCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404563	70323	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	317	9	0	3	3.0	CCN(CC)CC(CCCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL194464	70323	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	317	9	0	3	3.0	CCN(CC)CC(CCCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44397123	127560	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	616	12	3	6	4.1	CN(C)c1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL366334	127560	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	616	12	3	6	4.1	CN(C)c1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44400825	124323	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	638	12	2	7	6.5	O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL363561	124323	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	638	12	2	7	6.5	O=C(N[C@H](Cc1csc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		11295536	57540	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL166328	57540	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	2	5	3.4	COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		11364802	165289	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL423250	165289	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	545	7	2	5	3.5	CN(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44412687	79435	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	10	4	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211364	79435	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	10	4	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44444430	94322	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	440	5	1	4	3.6	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250575	94322	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	440	5	1	4	3.6	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44444442	154650	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	0	4	6.2	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)CC(C)C	10.1016/j.bmcl.2007.06.088
		CHEMBL399487	154650	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	0	4	6.2	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)CC(C)C	10.1016/j.bmcl.2007.06.088
		44447246	155516	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL404206	155516	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44415925	81106	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	523	8	1	4	6.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CC(C)C(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215609	81106	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	523	8	1	4	6.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CC(C)C(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44434611	88614	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	373	6	2	2	3.9	NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL235627	88614	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	373	6	2	2	3.9	NCCCN(C(=O)/C=C/c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		10270570	89033	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	6	2	2	4.4	CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236450	89033	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	6	2	2	4.4	CC(c1ccc2ccccc2c1)N(CCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434850	89174	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL236645	89174	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1ccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		44434683	89303	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	10	3	3	4.9	C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		CHEMBL236847	89303	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	10	3	3	4.9	C/C(=C\c1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		44434859	90034	0	None	-6	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL238158	90034	0	None	-6	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)C1	10.1016/j.bmc.2007.06.003
		44432895	86940	1	None	-	1	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL232327	86940	1	None	-	1	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		168293053	192066	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5202611	192066	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2980	98	36	38	-8.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL438596	213781	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44404550	72560	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL199192	72560	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		11851038	140335	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL3644337	211977	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644337	211977	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		11851038	140335	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		46885972	8119	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		CHEMBL1091631	8119	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	3	4.4	CC(C)N1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		CHEMBL5075712	214394	0	None	-77	3	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137659790	159322	0	None	-5	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4099889	159322	0	None	-5	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		89007938	144394	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1059	19	17	12	-3.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3906011	144394	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1059	19	17	12	-3.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644299	211942	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44444429	94321	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	439	5	0	4	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250573	94321	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	439	5	0	4	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		16132144	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		168273045	190254	0	None	1	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	62	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5175392	190254	0	None	1	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	62	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168285101	191644	0	None	-16	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5195937	191644	0	None	-16	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccccc2CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44432895	86940	1	None	-	1	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL232327	86940	1	None	-	1	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	511	13	2	8	4.9	COc1cc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		4189	206922	96	None	-46	34	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL1559	206922	96	None	-46	34	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL91	206922	96	None	-46	34	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
		CHEMBL409049	212745	0	None	12	3	Human	7.9	pKi	=	7.9	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1C(=O)NCC(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)CSSC1(C)C	10.1021/jm030119t
		44433300	151433	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	12	2	5	5.0	CC(C)C[C@H](NC(=O)CCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396186	151433	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	12	2	5	5.0	CC(C)C[C@H](NC(=O)CCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11181804	128507	0	None	21	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.08.055
		CHEMBL366706	128507	0	None	21	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	641	11	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644332	211972	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644295	211938	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3644310	211950	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3644332	211972	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44393888	127082	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL365636	127082	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	625	10	3	6	4.9	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44433423	88724	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL236110	88724	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44433428	89327	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)C3CN(C4CCOCC4)CC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL236910	89327	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)C3CN(C4CCOCC4)CC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		24873537	146061	0	None	20	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL391902	146061	0	None	20	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44433423	88724	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL236110	88724	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		44412897	139232	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378866	139232	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44416213	80221	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213721	80221	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44432903	87193	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232724	87193	1	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	519	14	1	6	6.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44447791	155317	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL403047	155317	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44443014	154010	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398409	154010	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25133210	169457	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
		CHEMBL442829	169457	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	615	11	3	5	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1CCCN1	10.1021/jm800525p
		44397283	67166	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187659	67166	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397304	126826	0	None	158	4	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365465	126826	0	None	158	4	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	6	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44412509	140177	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	12	3	5	5.4	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CNC2CCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL380391	140177	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	12	3	5	5.4	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CNC2CCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		168281681	190755	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5182977	190755	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		168289584	191786	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3108	98	37	41	-6.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5198158	191786	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3108	98	37	41	-6.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		24886260	12299	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	579	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184895	12299	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	579	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL376999	12299	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	579	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		9851816	11822	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	10	2	5	5.0	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182091	11822	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	10	2	5	5.0	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211260	11822	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	10	2	5	5.0	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C(C)C)CC1	10.1016/j.bmcl.2006.04.016
		44433274	151704	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	12	1	5	5.3	CC(C)C[C@H](NCCN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396431	151704	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	12	1	5	5.3	CC(C)C[C@H](NCCN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44562400	175184	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL457059	175184	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44322959	156075	0	None	-5	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL406276	156075	0	None	-5	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	21	9	7	0.6	CCCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391271	63849	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	644	11	3	7	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL180304	63849	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	644	11	3	7	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44391381	65570	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.2	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)C2CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183134	65570	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.2	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)C2CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		44396079	127294	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	562	11	4	6	3.5	CC(NCc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL365874	127294	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	562	11	4	6	3.5	CC(NCc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44393809	66178	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL184325	66178	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	11	4	6	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCO)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44433385	89055	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236489	89055	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	612	8	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44405377	72024	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197541	72024	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	644	12	3	6	3.5	NC(Cc1ccncc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44447245	94674	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL252622	94674	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		44447214	169030	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	555	6	1	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL439427	169030	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	555	6	1	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416228	80005	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212802	80005	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44415984	80517	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL214799	80517	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		9842665	156806	12	None	-3	2	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44447778	155416	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403676	155416	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44396953	66883	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	3	7	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL186370	66883	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	3	7	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL427629	213357	0	None	-5	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		44562413	175182	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	12	1	4	6.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC(C)C)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL457058	175182	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	12	1	4	6.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC(C)C)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44412864	79694	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	3	7	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Oc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211540	79694	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	3	7	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Oc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		44444441	94026	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	0	4	5.0	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL248767	94026	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	0	4	5.0	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44412791	138809	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	3	7	1.4	COCC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378105	138809	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	3	7	1.4	COCC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44444440	155131	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	468	6	0	4	4.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL402059	155131	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	468	6	0	4	4.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44434855	90030	0	None	-2	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	90030	0	None	-2	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44442899	93699	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	446	5	1	4	3.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247045	93699	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	446	5	1	4	3.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44442985	93767	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	589	8	1	5	5.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cc5ccccc5n4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247411	93767	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	589	8	1	5	5.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cc5ccccc5n4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		10180932	89407	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	11	2	2	5.8	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237051	89407	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	11	2	2	5.8	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10159196	89738	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	11	2	4	4.4	NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237694	89738	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	11	2	4	4.4	NCCCCCN(Cc1ccc2c(c1)OCO2)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434780	148172	0	None	-2	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	525	8	2	2	7.3	NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393568	148172	0	None	-2	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	525	8	2	2	7.3	NC1CCC(CC2CCC(N(C(=O)CCCc3c[nH]c4ccccc34)C3CCc4ccccc4C3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44413829	78066	0	None	1	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL210011	78066	0	None	1	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		168288992	191770	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5197875	191770	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		70660697	152035	0	None	-616	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3967140	152035	0	None	-616	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	834	16	12	10	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](CCCN)NC1=O	nan
		44415956	141956	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
		CHEMBL387246	141956	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1016/j.bmcl.2006.05.087
		44415956	141956	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		CHEMBL387246	141956	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	13	6	5	0.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		168288992	191770	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5197875	191770	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3030	98	37	39	-8.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44404545	72297	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC)C(=O)C(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198319	72297	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	307	5	0	3	2.0	CCN(CC)C(=O)C(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		11851038	140335	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44393808	66131	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL184068	66131	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	574	10	4	6	2.5	NCCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL3667953	212147	0	None	77	2	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(=O)O)NC1=O	nan
		44432900	87192	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232723	87192	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		168274920	190263	0	None	-11	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5175444	190263	0	None	-11	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2cccc(c2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		1338	3807	43	None	53	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44409104	76525	0	None	2	3	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		CHEMBL206033	76525	0	None	2	3	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	582	12	5	5	2.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		44410175	168992	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL439158	168992	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	7	3	3	3.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC1CCNCC1	10.1016/j.bmcl.2006.01.016
		44562439	179040	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471339	179040	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44562286	188990	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CNC)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508641	188990	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.6	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CNC)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644299	211942	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646873	212012	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646884	212022	0	None	53	2	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644299	211942	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646873	212012	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646884	212022	0	None	53	2	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667927	212121	0	None	776	2	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44393864	66196	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL184405	66196	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(N[C@H]1CCCCC1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		11786860	66334	1	None	45	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185035	66334	1	None	45	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	614	9	4	6	3.4	CC(N[C@H]1CCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		16007285	81122	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215659	81122	0	None	13	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CCC(C)[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444500	94144	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL249370	94144	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	9	2	5	4.4	CC(C)[C@H](NC(=O)CCN)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44444483	155657	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	524	7	0	4	5.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL404854	155657	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	524	7	0	4	5.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.06.088
		44397283	67166	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187659	67166	0	None	112	3	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44412641	78022	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	12	2	5	4.9	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209825	78022	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	12	2	5	4.9	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		44412640	139563	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.9	CCN(CC)CC(C1CCCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379719	139563	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.9	CCN(CC)CC(C1CCCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL427666	213364	0	None	-4	4	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CSC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(N)=O	10.1021/jm0501432
		168281969	191278	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5190661	191278	0	None	2	4	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5083551	214869	0	None	-14	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44405368	71962	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197328	71962	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.1	NC(Cc1ccccc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44405582	72470	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	10	2	4	4.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198916	72470	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	10	2	4	4.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447209	94576	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	638	10	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL251966	94576	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	638	10	1	5	6.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447211	94579	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	8	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL251983	94579	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	8	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412884	139448	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	11	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL379400	139448	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	11	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		16132144	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44432900	87192	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232723	87192	1	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.3	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCCN)cc1	10.1016/j.bmcl.2007.06.010
		44447787	155270	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL402838	155270	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442944	93600	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL246606	93600	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	543	8	1	6	4.9	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443024	94122	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(C(F)(F)F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL249268	94122	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(C(F)(F)F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404562	71424	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	303	8	0	3	2.6	CCN(CC)CC(CCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL195998	71424	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	303	8	0	3	2.6	CCN(CC)CC(CCc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL2370965	209968	0	None	1	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@](C)(Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44347081	168627	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL436169	168627	0	None	3	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		11237444	127465	0	None	-245	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
		CHEMBL366042	127465	0	None	-245	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	503	8	4	3	5.4	CC(C)(N)C/N=C(\Nc1ccc(C(=O)NCCc2ccc(Cl)cc2Cl)cc1)NC1CCCCC1	10.1021/jm0400496
		11214733	120296	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL352677	120296	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	530	7	2	4	4.0	CCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		46930942	68403	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	782	24	10	8	1.5	[N-]=[N+]=NCCCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2011.08.053
		CHEMBL1917057	68403	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	782	24	10	8	1.5	[N-]=[N+]=NCCCCCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2011.08.053
		122178161	121255	0	None	-	1	Mouse	5.9	pKi	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577990	121255	0	None	-	1	Mouse	5.9	pKi	=	5.9	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	962	11	10	10	-1.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44412881	77030	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	563	10	4	6	2.3	CC(C)NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL207166	77030	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	563	10	4	6	2.3	CC(C)NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44412688	138196	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	627	11	4	7	3.4	COc1ccccc1NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL376974	138196	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	627	11	4	7	3.4	COc1ccccc1NC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44434758	88694	0	None	-1	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	755	14	3	5	9.6	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL236002	88694	0	None	-1	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	755	14	3	5	9.6	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44443040	93650	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	0	6	5.7	COc1ccc(CN(CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)OC)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL246807	93650	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	0	6	5.7	COc1ccc(CN(CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)OC)cc1	10.1016/j.bmcl.2007.10.032
		44443042	93926	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	0	5	5.5	CCN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL248224	93926	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	9	0	5	5.5	CCN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44347750	16415	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	7	0	3	6.2	CCCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		CHEMBL123113	16415	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	7	0	3	6.2	CCCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		10157774	89301	0	None	-8	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236842	89301	0	None	-8	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434657	90234	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL238341	90234	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		168272746	190524	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5179536	190524	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		176	398	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2157	398	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		2566	398	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		CHEMBL633	398	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		DB01118	398	66	None	-6	31	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
		88944286	143031	0	None	-660	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	981	19	14	11	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3894840	143031	0	None	-660	2	Human	5.9	pKi	=	5.9	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	981	19	14	11	-2.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		168283887	191020	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186784	191020	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2205	73	27	29	-5.8	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)O	10.1021/acs.jmedchem.2c00786
		168276817	190098	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5172843	190098	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		2247	505	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		249	505	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		2603	505	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		CHEMBL296419	505	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		DB00637	505	81	None	-147	42	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
		16132144	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		11845276	80053	0	None	2	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
		CHEMBL212976	80053	0	None	2	3	Human	6.9	pKi	=	6.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	14	4	4	4.9	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)CCc1ccccc1	10.1021/jm060384p
		CHEMBL438596	213781	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		11847312	79762	0	None	-2	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		CHEMBL211798	79762	0	None	-2	3	Human	5.9	pKi	=	5.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	613	12	6	6	1.8	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		168276817	190098	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5172843	190098	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3114	101	37	39	-7.3	CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44401440	70120	0	None	1	2	Human	6.9	pKi	=	6.9	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL194011	70120	0	None	1	2	Human	6.9	pKi	=	6.9	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL5091236	215299	0	None	-173	3	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44400711	71112	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	594	11	2	6	4.2	CS(=O)(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195414	71112	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	594	11	2	6	4.2	CS(=O)(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44410379	141203	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
		CHEMBL382833	141203	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	486	13	2	5	4.2	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(OC)cc(OC)c1	10.1016/j.bmcl.2006.01.016
		44395681	66870	0	None	70	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	13	3	6	3.8	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186289	66870	0	None	70	4	Human	7.9	pKi	=	7.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	13	3	6	3.8	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644325	211965	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3644325	211965	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		168281681	190755	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5182977	190755	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2878	98	37	37	-7.4	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O	10.1021/acs.jmedchem.2c00786
		44394080	126766	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL365279	126766	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccc(F)c2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		24741624	138380	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL377231	138380	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL267492	210724	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432953	148641	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393948	148641	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		24741624	138380	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
		CHEMBL377231	138380	0	None	6	3	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1021/jm701137s
		11847001	80228	0	None	138	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL213747	80228	0	None	138	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		25132864	172602	0	None	12	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
		CHEMBL449050	172602	0	None	12	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	590	12	2	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)COC	10.1021/jm800525p
		25129108	172696	0	None	15	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
		CHEMBL450236	172696	0	None	15	3	Human	7.9	pKi	=	7.9	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CCCC1	10.1021/jm800525p
		44404549	140518	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL381015	140518	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)C[C@H](c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		11157584	168244	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL433710	168244	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.08.018
		44412626	79935	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	10	1	4	5.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)N2CCc3ccccc3C2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL212535	79935	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	10	1	4	5.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)N2CCc3ccccc3C2)CC1	10.1016/j.bmcl.2006.04.002
		44432953	148641	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393948	148641	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	556	13	2	5	7.7	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccc4[nH]ccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44416375	81076	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL215481	81076	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		44433278	148447	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	2	5	4.2	CC(C)C[C@H](NCC(N)=O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393789	148447	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	11	2	5	4.2	CC(C)C[C@H](NCC(N)=O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44322977	111569	0	None	-2	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL328117	111569	0	None	-2	3	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	714	18	11	8	-1.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391303	65317	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	631	11	2	7	3.4	CCOC(=O)CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL182900	65317	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	631	11	2	7	3.4	CCOC(=O)CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44396102	66733	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	537	11	3	6	3.5	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL185725	66733	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	537	11	3	6	3.5	CC(NCc1ccco1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44395920	96799	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	581	13	3	6	4.4	CCC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL264983	96799	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	581	13	3	6	4.4	CCC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		11753667	57178	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164857	57178	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	4.0	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL3644301	211944	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		134143956	150552	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	17	17	12	1.5	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)O)/N=C\1O	nan
		CHEMBL3954833	150552	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	17	17	12	1.5	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H]([C@H](C)O)/N=C\1O	nan
		44405549	71882	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	578	10	2	4	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197075	71882	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	578	10	2	4	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44415433	81232	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215851	81232	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405378	140565	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		CHEMBL381197	140565	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.1	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)Cc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		44416375	81076	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215481	81076	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44442990	93706	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	4	6.2	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL247088	93706	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	584	9	1	4	6.2	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44443017	154141	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4C(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398542	154141	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	604	8	1	4	6.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4C(F)(F)F)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44347765	16768	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	5	0	3	5.3	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)c(C)n1C	10.1016/j.bmcl.2004.05.003
		CHEMBL124410	16768	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	5	0	3	5.3	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)c(C)n1C	10.1016/j.bmcl.2004.05.003
		71458058	79047	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	625	8	3	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CCC2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113152	79047	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	625	8	3	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CCC2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		11477853	66894	0	None	-38	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
		CHEMBL186439	66894	0	None	-38	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	7	3	3	5.2	CNC1CCN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)C1	10.1021/jm0400496
		44562365	176135	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	575	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL459217	176135	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	575	14	1	4	7.2	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44393421	123103	0	None	4	4	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	508	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL361052	123103	0	None	4	4	Human	5.9	pKi	=	5.9	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	508	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44444465	94231	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	7	2	5	5.3	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3ccccc3N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249986	94231	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	531	7	2	5	5.3	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3ccccc3N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44415537	139673	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccccc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL379792	139673	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccccc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		44265715	10185	0	None	-4	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL1159702	10185	0	None	-4	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		44434661	88513	0	None	-3	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	415	11	2	3	4.4	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL235136	88513	0	None	-3	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	415	11	2	3	4.4	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc(-c2ccccc2)cc1	10.1016/j.bmc.2007.06.003
		44434761	89167	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	625	11	3	3	8.9	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236626	89167	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	625	11	3	3	8.9	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434647	89590	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.3	NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3	10.1016/j.bmc.2007.06.003
		CHEMBL237483	89590	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.3	NCCCCCN(C(=O)CCCc1c[nH]c2ccccc12)C1C2CC3CC(C2)CC1C3	10.1016/j.bmc.2007.06.003
		44434605	149514	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	356	10	1	3	4.4	C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1	10.1016/j.bmc.2007.06.003
		CHEMBL394647	149514	0	None	-2	4	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	356	10	1	3	4.4	C/C(=C\c1ccccc1)CN(CCCN)C(=O)CCCc1cccs1	10.1016/j.bmc.2007.06.003
		137660671	159218	0	None	-147	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4098785	159218	0	None	-147	3	Human	5.9	pKi	=	5.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1708	20	19	21	-2.8	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		137636677	156100	0	None	-28	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4063111	156100	0	None	-28	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		168272746	190524	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5179536	190524	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2674	88	33	35	-8.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL3644287	211931	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644287	211931	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644281	211925	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644281	211925	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		88590642	125067	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		CHEMBL3644360	125067	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		88590642	125067	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		CHEMBL3644360	125067	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1113	19	18	13	-4.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CNC(=O)[C@H]2CCNC2)NC1=O	nan
		44393823	123974	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL362880	123974	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	676	9	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCN(c3ccccc3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		2726	919	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		621	919	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		83	919	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		CHEMBL71	919	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		DB00477	919	68	None	-154	72	Human	4.8	pKi	=	4.8	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
		44412511	77940	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC)C(=O)C(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209558	77940	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC)C(=O)C(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL438596	213781	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		11180881	66821	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2005.03.053
		CHEMBL186074	66821	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2005.03.053
		44562399	176963	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	10	2	5	4.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462346	176963	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	10	2	5	4.9	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		11180881	66821	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186074	66821	1	None	47	4	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCNC1	10.1016/j.bmcl.2004.08.055
		88590610	125060	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644306	125060	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644315	211955	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O	nan
		CHEMBL3644349	211988	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3646872	212011	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590610	125060	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644306	125060	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3644315	211955	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O	nan
		CHEMBL3644349	211988	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3646872	212011	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88287712	127561	0	None	36	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1154	19	17	12	-1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3663364	127561	0	None	36	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1154	19	17	12	-1.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](Cc2cccc(C(N)=O)c2)NC1=O	nan
		CHEMBL3663373	212102	0	None	9	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL2415081	210432	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		CHEMBL2415083	210434	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		168281969	191278	0	None	2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5190661	191278	0	None	2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3072	100	37	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433442	90185	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	5	1	5	5.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL238197	90185	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	5	1	5	5.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)OC(C)(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44412911	168994	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	12	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL439168	168994	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	12	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL5080489	214689	0	None	-1	3	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44322787	105964	0	None	-1	3	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL312998	105964	0	None	-1	3	Human	7.8	pKi	=	7.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	791	21	11	8	0.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C(O)Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		24886499	11821	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	593	10	2	5	4.6	CCN1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182090	11821	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	593	10	2	5	4.6	CCN1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211202	11821	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	593	10	2	5	4.6	CCN1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44562596	174456	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	545	10	1	5	5.1	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL455394	174456	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	545	10	1	5	5.1	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		44322987	96732	0	None	-4	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL264306	96732	0	None	-4	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	20	9	7	0.2	CCCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44396158	67169	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	10	4	6	3.0	CC(N[C@@H]1CCCC[C@H]1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL187690	67169	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	10	4	6	3.0	CC(N[C@@H]1CCCC[C@H]1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL2415018	210429	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44405558	71790	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	12	2	4	4.8	CCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL196758	71790	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	12	2	4	4.8	CCCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44404566	70551	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1cccc(C(F)(F)F)c1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL194761	70551	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1cccc(C(F)(F)F)c1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404575	72521	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1c(F)cccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL199071	72521	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	311	6	0	3	2.6	CCN(CC)CC(c1c(F)cccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		71454508	79043	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	3	5	3.5	CNC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113148	79043	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	3	5	3.5	CNC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		71450912	78972	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	588	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL2113033	78972	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	588	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		11341046	66880	0	None	-57	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	7	4	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1	10.1021/jm0400496
		CHEMBL186339	66880	0	None	-57	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	7	4	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N\C2CCNC2)NC2CCCCC2)cc1	10.1021/jm0400496
		44392535	64272	0	None	-2	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	8	2	7	2.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL180937	64272	0	None	-2	4	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	8	2	7	2.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(Cn3cncn3)CCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44415765	81138	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	7	1	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc3c(c2)OCO3)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215697	81138	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	7	1	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc3c(c2)OCO3)CC1	10.1016/j.bmcl.2006.05.088
		44412677	138668	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.1	COc1ccc(C(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL377761	138668	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.1	COc1ccc(C(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		44412931	140995	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	12	5	8	0.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(CO)CO)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL382353	140995	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	12	5	8	0.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(CO)CO)CC1	10.1016/j.bmcl.2006.04.069
		44416025	79967	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	533	7	1	4	6.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CSc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212664	79967	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	533	7	1	4	6.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CSc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44434696	149198	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	11	3	3	8.4	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL394394	149198	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	11	3	3	8.4	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434762	153010	0	None	1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL397550	153010	0	None	1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44443044	93889	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	8	0	5	5.1	CC(=O)N(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL248057	93889	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	8	0	5	5.1	CC(=O)N(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44347987	164338	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	5	1	2	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.05.003
		CHEMBL421254	164338	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	5	1	2	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc[nH]1	10.1016/j.bmcl.2004.05.003
		44265707	10184	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	354	10	3	4	2.1	C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL1159701	10184	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	354	10	3	4	2.1	C=CCOC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		71454518	79150	0	None	-10	4	Human	4.8	pKi	=	4.8	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	456	10	4	3	3.3	NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL2113315	79150	0	None	-10	4	Human	4.8	pKi	=	4.8	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	456	10	4	3	3.3	NC(N)=NCCC[C@H](N)C(=O)N(CCc1c[nH]c2ccccc12)Cc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		9842665	156806	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44404543	72376	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	4	1.4	CCN(CC(c1ccccc1F)N1CCN(C)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.08.018
		CHEMBL198607	72376	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	4	1.4	CCN(CC(c1ccccc1F)N1CCN(C)CC1)S(C)(=O)=O	10.1016/j.bmcl.2005.08.018
		44413879	138902	0	None	-123	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL378293	138902	0	None	-123	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	681	15	6	7	0.9	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL5081077	214717	0	None	-32	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CN1C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]1CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137647538	157962	0	None	-275	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4084765	157962	0	None	-275	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44400708	68681	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	12	2	7	5.9	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1nccs1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL192153	68681	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	613	12	2	7	5.9	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1nccs1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562457	189333	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL512496	189333	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		122178157	121252	0	None	50	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577986	121252	0	None	50	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		122178164	121258	0	None	158	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577993	121258	0	None	158	2	Mouse	7.8	pKi	=	7.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		11636019	72360	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198535	72360	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44405426	135786	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL373037	135786	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	11	3	5	4.7	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3Cc4ccccc4CN3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44416201	141628	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL385274	141628	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44447785	95077	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255313	95077	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443032	94159	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	1	6	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(OC)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL249473	94159	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	596	10	1	6	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c(OC)c1	10.1016/j.bmcl.2007.10.032
		9842665	156806	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmcl.2005.03.053
		CHEMBL40711	156806	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1016/j.bmcl.2005.03.053
		44322958	107012	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL315356	107012	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	727	18	9	7	0.4	CC(C)(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44323033	107152	0	None	-5	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL316259	107152	0	None	-5	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	747	19	10	7	0.9	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44322788	157383	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL407825	157383	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	699	19	9	7	-0.2	CCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391272	131795	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	670	12	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL369348	131795	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	670	12	3	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		10033237	69071	0	None	-933	3	Human	6.8	pKi	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm201226w
		CHEMBL1923662	69071	0	None	-933	3	Human	6.8	pKi	=	6.8	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm201226w
		CHEMBL3577977	211745	0	None	3	2	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577979	211747	0	None	8	2	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577982	211750	0	None	3	2	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577988	211751	0	None	-	1	Mouse	6.8	pKi	=	6.8	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44433422	88723	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	562	6	1	4	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236109	88723	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	562	6	1	4	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415453	80227	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CCC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213739	80227	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CCC(C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405553	158143	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	2	4	4.0	CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL408721	158143	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	552	10	2	4	4.0	CCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44416163	141785	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	457	8	1	4	4.9	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(Cl)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL386162	141785	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	457	8	1	4	4.9	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(Cl)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		9842665	156806	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		70681743	75080	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	542	10	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		CHEMBL2035942	75080	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	542	10	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		44447774	155214	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	468	5	1	4	4.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL402588	155214	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	468	5	1	4	4.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44444462	94203	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	517	7	1	5	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3cccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249780	94203	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	517	7	1	5	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNc3cccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44415766	138732	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	2	3	5.8	Cc1[nH]c2ccccc2c1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL378016	138732	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	2	3	5.8	Cc1[nH]c2ccccc2c1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		44416228	80005	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212802	80005	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434766	154714	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL399810	154714	0	None	-1	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44348035	113788	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	412	6	0	3	5.8	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C(C)C)cn1C	10.1016/j.bmcl.2004.05.003
		CHEMBL332382	113788	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	412	6	0	3	5.8	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C(C)C)cn1C	10.1016/j.bmcl.2004.05.003
		71456250	79027	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	557	6	3	5	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113132	79027	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	557	6	3	5	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		23653113	88652	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	9	4	2	4.2	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235798	88652	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	427	9	4	2	4.2	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10293285	89612	0	None	-2	3	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	382	7	1	2	4.9	NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL237528	89612	0	None	-2	3	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	382	7	1	2	4.9	NCCCN(Cc1ccc2ccccc2c1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		10137615	89736	0	None	-6	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	9	2	2	5.4	CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237692	89736	0	None	-6	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	9	2	2	5.4	CC(c1ccc(C(F)(F)F)cc1)N(CCCCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10108894	89737	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	355	8	2	2	4.4	NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1	10.1016/j.bmc.2007.06.003
		CHEMBL237693	89737	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	355	8	2	2	4.4	NCCCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCCCCC1	10.1016/j.bmc.2007.06.003
		44434652	89901	0	None	-7	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	403	12	2	2	5.2	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237912	89901	0	None	-7	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	403	12	2	2	5.2	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434614	151584	1	None	1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.9	NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL396341	151584	1	None	1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.9	NCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434857	154427	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	475	13	2	4	3.9	NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL398980	154427	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	475	13	2	4	3.9	NCCCN1CCN(CCCN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		88944293	153715	0	None	-6606	2	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	15	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3981581	153715	0	None	-6606	2	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	15	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		168295726	192405	0	None	-263	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5207936	192405	0	None	-263	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2547	50	34	33	-2.8	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCOCCC(=O)O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL3644339	211979	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644339	211979	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		168276294	190508	0	None	-79	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	3264	55	36	40	1.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5179373	190508	0	None	-79	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	3264	55	36	40	1.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5nnn(CC(=O)N6CCCC[C@H]6C6(O)CN(C(=O)c7ccc(F)c(F)c7Nc7ccc(I)cc7F)C6)c5CCC43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44447780	95044	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255100	95044	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442995	93652	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL246837	93652	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	562	8	1	4	5.9	O=C([C@H]1CN(C2CCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44413914	139518	0	None	-26	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL379508	139518	0	None	-26	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44444505	94508	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL251594	94508	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	649	10	1	5	5.9	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44410802	140385	0	None	114	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	1	5	5.3	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380858	140385	0	None	114	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	1	5	5.3	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2c3ccccc3CN2C)CC1	10.1016/j.bmcl.2005.10.103
		44432955	87207	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232773	87207	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44322957	206211	0	None	-2	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL86573	206211	0	None	-2	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	753	19	10	7	0.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CC(F)(F)F)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL88185	215896	0	None	1	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CS(=O)(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		11753668	120369	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL353239	120369	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	596	8	2	6	3.8	Cn1ccnc1Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44405443	72581	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	568	11	2	5	3.2	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL199273	72581	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	568	11	2	5	3.2	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44413005	79889	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	3	6	2.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCC(F)(F)F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL212358	79889	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	3	6	2.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCC(F)(F)F)CC1	10.1016/j.bmcl.2006.04.069
		44447222	94618	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	10	1	6	5.1	CC(C)C[C@H](NCCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252234	94618	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	10	1	6	5.1	CC(C)C[C@H](NCCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44415434	138485	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL377480	138485	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447210	154882	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	624	10	2	5	6.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400738	154882	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	624	10	2	5	6.0	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		71454509	79045	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	627	9	2	5	4.6	CCN(CC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113150	79045	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	627	9	2	5	4.6	CCN(CC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44323212	168719	0	None	-1	2	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		CHEMBL436903	168719	0	None	-1	2	Human	5.8	pKi	=	5.8	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	787	9	10	8	-1.0	C[C@@H]1NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	10.1021/jm020021z
		44562283	188916	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	573	14	0	4	7.4	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL507776	188916	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	573	14	0	4	7.4	CCCCN(CCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		11272336	57194	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164969	57194	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	517	6	3	5	3.0	Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		11364343	119924	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL349427	119924	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	516	6	2	4	3.7	Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44444431	94371	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	7	1	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNS(C)(=O)=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250778	94371	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	7	1	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNS(C)(=O)=O)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44415370	168940	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL438793	168940	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44416214	80023	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212882	80023	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44434689	89175	0	None	-14	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	14	2	2	5.9	NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236649	89175	0	None	-14	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	431	14	2	2	5.9	NCCCCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434635	168887	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	363	10	2	2	4.3	NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL438334	168887	0	None	-1	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	363	10	2	2	4.3	NCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44432891	87801	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233809	87801	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL3644335	211975	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134145039	150609	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	18	17	12	2.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCN)/N=C\1O	nan
		CHEMBL3955264	150609	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1031	18	17	12	2.1	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCN)/N=C\1O	nan
		44413969	80230	0	None	-5	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL213752	80230	0	None	-5	3	Human	5.8	pKi	=	5.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL3644281	211925	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644281	211925	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		46885526	7764	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
		CHEMBL1089135	7764	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
		CHEMBL1204056	7764	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	456	4	1	5	3.2	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)C1CC1	10.1021/jm9017866
		CHEMBL438596	213781	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		46885761	8028	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
		CHEMBL1090813	8028	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1F	10.1021/jm9017866
		10304794	139405	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	139405	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44432891	87801	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233809	87801	1	None	-	1	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	483	13	2	8	4.4	CCCN(CCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		44400707	68313	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	570	12	2	5	5.6	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCC1CC1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191645	68313	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	570	12	2	5	5.6	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCC1CC1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400658	68638	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	559	12	3	6	4.2	NCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191831	68638	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	559	12	3	6	4.2	NCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562288	174250	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454901	174250	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		24180592	97013	0	None	-5	6	Mouse	7.8	pKi	=	7.8	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		CHEMBL266647	97013	0	None	-5	6	Mouse	7.8	pKi	=	7.8	Binding	Binding affinity to mouse MC4RBinding affinity to mouse MC4R	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		CHEMBL3663360	212090	0	None	91	2	Human	7.8	pKi	=	7.8	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		CHEMBL2415019	210430	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCCc1cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44433444	90186	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	7	1	5	5.2	CCN1CCC(N2C[C@@H](C(=O)N3CCN(c4ccc(C)cc4[C@@H](N)C(C)C)CC3)[C@H](c3ccc(Cl)cc3)C2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL238198	90186	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	7	1	5	5.2	CCN1CCC(N2C[C@@H](C(=O)N3CCN(c4ccc(C)cc4[C@@H](N)C(C)C)CC3)[C@H](c3ccc(Cl)cc3)C2)CC1	10.1016/j.bmcl.2007.09.079
		44433445	168974	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	1	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(C(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL439040	168974	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	1	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(C(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44415693	79848	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CCC(C)[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212192	79848	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CCC(C)[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444510	155132	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL402060	155132	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	647	9	2	5	5.6	CC(C)C[C@H](NC(=O)C1CNC1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL267492	210724	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432955	87207	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232773	87207	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	14	1	5	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(NCc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44447780	95044	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255100	95044	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44447803	95065	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	546	6	1	5	5.3	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL255261	95065	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	546	6	1	5	5.3	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44413931	78015	0	None	1	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL209789	78015	0	None	1	3	Human	7.8	pKi	=	7.8	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	16	5	6	1.9	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44397029	67105	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	661	13	3	7	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1OC	10.1016/j.bmcl.2005.05.017
		CHEMBL187390	67105	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	661	13	3	7	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1OC	10.1016/j.bmcl.2005.05.017
		44397282	123421	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	573	11	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL361693	123421	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	573	11	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44412613	138926	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL378411	138926	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	633	10	2	6	4.0	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CN2C(=O)CCC2=O)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		44412646	139269	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	552	11	2	4	5.4	CC(C)CC(CC(C)C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379051	139269	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	552	11	2	4	5.4	CC(C)CC(CC(C)C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		10304794	139405	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	139405	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL89270	215899	0	None	-3	3	Human	6.8	pKi	=	6.8	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1016/s0960-894x(03)00552-3
		44433386	88531	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	8	2	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(CCN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235215	88531	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	565	8	2	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(CCN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44412912	79878	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	521	10	2	6	2.9	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL212308	79878	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	521	10	2	6	2.9	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)=O)CC1	10.1016/j.bmcl.2006.04.069
		44447225	94921	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	2	6	4.3	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254279	94921	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	2	6	4.3	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44405374	135273	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3ccccc3F)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL372621	135273	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3ccccc3F)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447230	154889	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.5	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400787	154889	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	608	9	2	6	4.5	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44577056	187758	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	413	6	1	3	4.5	CC(C)[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL495674	187758	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	413	6	1	3	4.5	CC(C)[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44447816	95409	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256955	95409	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443003	153861	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	590	8	1	4	5.7	O=C(C1CCCC1)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398285	153861	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	590	8	1	4	5.7	O=C(C1CCCC1)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25132524	176758	0	None	5	3	Human	6.8	pKi	=	6.8	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		CHEMBL460349	176758	0	None	5	3	Human	6.8	pKi	=	6.8	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	504	8	2	4	2.7	CC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		9977350	16294	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1ncc(C)n1C	10.1016/j.bmcl.2004.05.003
		CHEMBL122491	16294	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1ncc(C)n1C	10.1016/j.bmcl.2004.05.003
		44347980	16438	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	430	5	0	3	5.7	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL123263	16438	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	430	5	0	3	5.7	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		71459942	79046	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	655	11	2	5	5.4	CCCN(CCC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113151	79046	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	655	11	2	5	5.4	CCCN(CCC)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44397079	127552	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	539	11	3	5	3.5	CC(C)CNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		CHEMBL366313	127552	0	None	-	1	Human	6.8	pKi	=	6.8	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	539	11	3	5	3.5	CC(C)CNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		44395646	67048	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	468	8	2	5	4.1	NC(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		CHEMBL187147	67048	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	468	8	2	5	4.1	NC(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		44415631	79939	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	1	4	5.9	CCC(C)[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212553	79939	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	1	4	5.9	CCC(C)[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44412684	138927	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	628	11	3	8	3.4	COc1ccccc1OC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378412	138927	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	628	11	3	8	3.4	COc1ccccc1OC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44412740	139278	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	3	7	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL379091	139278	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	3	7	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		44412676	169303	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	582	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL441532	169303	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	582	10	3	6	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		70681741	75077	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	492	10	2	4	2.8	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(F)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035939	75077	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	492	10	2	4	2.8	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(F)c1	10.1016/j.bmc.2012.04.001
		44447811	155034	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	462	5	1	4	3.7	CC(=O)N1CC[C@H](c2ccccc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401585	155034	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	462	5	1	4	3.7	CC(=O)N1CC[C@H](c2ccccc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443038	154891	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	622	11	0	5	6.8	COc1ccc(CN(CC(C)C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL400789	154891	0	None	-	1	Human	5.8	pKi	=	5.8	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	622	11	0	5	6.8	COc1ccc(CN(CC(C)C)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44434865	88750	0	None	-5	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	589	10	4	3	6.5	NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL236226	88750	0	None	-5	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	589	10	4	3	6.5	NC1CCCC(NC(=O)NC2CCCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		44434632	146309	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	10	2	2	4.4	NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL392096	146309	0	None	-2	4	Human	4.8	pKi	=	4.8	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	10	2	2	4.4	NCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		9842665	156806	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		88213487	142916	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1088	20	18	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3893834	142916	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1088	20	18	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3644340	211980	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)CNC(N)=O)NC1=O	nan
		44401573	71198	0	None	-1	2	Human	5.7	pKi	=	5.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	568	13	5	4	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL195638	71198	0	None	-1	2	Human	5.7	pKi	=	5.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	568	13	5	4	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		89703080	151910	0	None	-61	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	970	17	12	10	-0.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	nan
		CHEMBL3966157	151910	0	None	-61	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	970	17	12	10	-0.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O	nan
		44413830	77950	0	None	-1	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL209622	77950	0	None	-1	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44415991	80510	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL214770	80510	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1016/j.bmcl.2006.05.087
		44415991	80510	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
		CHEMBL214770	80510	0	None	21	3	Human	6.7	pKi	=	6.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	3	5	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN)C1=O	10.1021/jm800525p
		CHEMBL3644287	211931	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644300	211943	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646850	211995	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3646854	211998	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3cccc(Cl)c3)CN2C1=O	nan
		134153231	152562	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3cccc(Cl)c3)CN2C1=O	nan
		CHEMBL3971748	152562	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3cccc(Cl)c3)CN2C1=O	nan
		CHEMBL3644287	211931	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644300	211943	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646850	211995	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		1324	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		16154396	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		16197727	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		44285019	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		57514683	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		91898441	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		CHEMBL441738	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		DB04931	302	25	None	-3	4	Human	7.7	pKi	=	7.7	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		None	10.1021/jm201226w
		44393885	124387	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL363925	124387	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	8	3	6	3.6	C[C@H]1CN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)[C@@H](C)CN1	10.1016/j.bmcl.2004.06.059
		16007264	79720	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL211564	79720	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		16007264	79720	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL211564	79720	0	None	26	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	572	9	2	4	5.5	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		25132526	188923	0	None	43	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
		CHEMBL507876	188923	0	None	43	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	10	2	4	4.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)C	10.1021/jm800525p
		10408	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		5329	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		9941379	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		CHEMBL2070241	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		DB11653	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.2c00793
		168281421	190957	0	None	-346	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5185945	190957	0	None	-346	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2430	43	34	31	-3.4	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCN)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432959	87247	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232972	87247	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		46877881	201818	0	None	2	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL606990	201818	0	None	2	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	813	9	10	8	-0.3	N=C(N)NCCC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C(=O)CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		9983075	77308	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL208268	77308	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	490	8	2	3	3.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCN1CCCC1	10.1016/j.bmcl.2006.01.016
		44415522	81460	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	8	1	3	6.5	CCCCC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215974	81460	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	8	1	3	6.5	CCCCC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444460	94174	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	1	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CC3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249575	94174	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	1	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CC3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44447223	94619	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	10	2	6	4.6	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252235	94619	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	656	10	2	6	4.6	CNCCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447769	95612	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257828	95612	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44447805	155376	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL403431	155376	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44442999	94456	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	7	1	4	4.5	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251287	94456	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	7	1	4	4.5	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443001	94457	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	9	1	4	5.3	CCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251288	94457	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	9	1	4	5.3	CCCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443037	154890	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	0	5	6.1	CCN(Cc1ccc(OC)cc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL400788	154890	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	0	5	6.1	CCN(Cc1ccc(OC)cc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44404546	72134	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL197859	72134	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404572	133567	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	305	7	0	4	2.3	CCN(CC)CC(c1ccccc1OC)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL371105	133567	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	305	7	0	4	2.3	CCN(CC)CC(c1ccccc1OC)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		58777970	79036	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113141	79036	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44397308	67527	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	605	10	3	5	3.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189601	67527	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	605	10	3	5	3.8	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		11179914	120182	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL351705	120182	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	518	6	3	5	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2O)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		46930943	68405	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2011.08.053
		CHEMBL1917059	68405	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence methodDisplacement of Eu-DTAP-NDP-alpha-MSH-NH2 from MC4 receptor expressed in human HEK293 cells after 1 hr by time resolved fluorescence method	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2011.08.053
		44415709	81143	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	8	1	3	6.6	CN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215712	81143	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	529	8	1	3	6.6	CN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44434707	149547	0	None	1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL394667	149547	0	None	1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44434763	151343	0	None	-3	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	685	13	3	5	9.0	COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL396111	151343	0	None	-3	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	685	13	3	5	9.0	COc1cc(Cl)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434765	161771	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	643	11	3	3	9.1	NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL413982	161771	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	643	11	3	3	9.1	NC1CCC(CC2CCC(N(Cc3c(F)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434592	89515	0	None	-5	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237315	89515	0	None	-5	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	399	9	2	2	5.0	NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		168269216	189877	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169353	189877	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44320339	206123	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	410	9	1	2	6.0	NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		CHEMBL85918	206123	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	410	9	1	2	6.0	NCCCCCC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		44433293	144923	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL391028	144923	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.4	CC(C)C[C@H](NC(=O)CCN)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400934	70613	0	None	173	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	10	2	5	4.9	CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL194987	70613	0	None	173	4	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	587	10	2	5	4.9	CN(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400662	125168	0	None	478	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	13	3	6	4.5	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL364463	125168	0	None	478	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	601	13	3	6	4.5	NCCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44562475	186013	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	519	9	3	5	3.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL487043	186013	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	519	9	3	5	3.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44562402	188763	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	644	12	1	6	6.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL505442	188763	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	644	12	1	6	6.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644321	211961	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3646857	212001	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646858	212002	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590671	125529	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646870	125529	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590671	125529	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646870	125529	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1106	20	17	12	-2.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134134523	143787	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3901055	143787	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3646857	212001	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646858	212002	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88287608	127558	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1066	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663333	127558	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1066	18	17	12	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663326	212058	0	None	-1	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(F)c2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663353	212083	0	None	213	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3663356	212086	0	None	436	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3667915	212112	0	None	16	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3667938	212132	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667942	212136	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88944366	148021	0	None	-19	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3934498	148021	0	None	-19	2	Human	8.7	pKi	=	8.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2cccc3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44349471	16873	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		CHEMBL124954	16873	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	667	9	0	6	5.2	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)N2CCN(C(=O)OC(C)(C)C)CC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		44456184	155488	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL404069	155488	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	8	2	6	4.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		10077773	87267	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233135	87267	4	None	204	4	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44412612	138925	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL378408	138925	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		44432949	86790	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232161	86790	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44400809	68402	0	None	407	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	599	11	3	5	5.1	O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191701	68402	0	None	407	2	Human	8.7	pKi	=	8.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	599	11	3	5	5.1	O=C(NC1CC1)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44456137	155121	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
		CHEMBL402017	155121	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.2	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C3CCOCC3)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.10.115
		44432949	86790	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232161	86790	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	609	15	1	6	9.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Oc4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44443030	94126	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	1	5	6.2	CC(C)Oc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL249271	94126	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	1	5	6.2	CC(C)Oc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44432943	150230	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395226	150230	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL2370533	209868	0	None	9	3	Human	8.7	pKi	=	8.7	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CC(=O)O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm010165y
		44456183	98022	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272956	98022	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	9	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		23635108	144963	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635108	144963	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL391056	144963	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL391056	144963	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	10	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL267492	210724	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432943	150230	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395226	150230	0	None	-	1	Human	8.7	pKi	=	8.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	562	14	1	7	7.1	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc([N+](=O)[O-])cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL385556	212354	0	None	29	3	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		44434563	88699	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236015	88699	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	551	10	3	5	3.9	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		44433285	88616	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL235640	88616	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	601	11	2	5	4.3	CNCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400811	68641	0	None	416	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	615	10	3	5	5.7	CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL191857	68641	0	None	416	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	615	10	3	5	5.7	CC(C)(C)NC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400660	70730	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195071	70730	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL2415080	210431	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		44400660	70730	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL195071	70730	0	None	239	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	5	4.8	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL439128	213825	0	None	2	3	Human	8.6	pKi	=	8.6	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		44434555	89404	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237050	89404	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		24740419	148194	0	None	478	4	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		CHEMBL393584	148194	0	None	478	4	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	575	11	1	5	5.4	Cc1ccc([C@@H](CC(C)C)NC(=O)CCN(C)C)c(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		CHEMBL412494	212997	0	None	19	3	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		44433297	153046	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397582	153046	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	615	12	2	5	4.7	CNCCC(=O)N[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44432931	87753	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233757	87753	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432931	87753	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233757	87753	0	None	-	1	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.8	CCC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44400777	68672	0	None	295	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	630	13	2	7	4.7	COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL192090	68672	0	None	295	2	Human	8.6	pKi	=	8.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	630	13	2	7	4.7	COC(=O)CCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44410176	76024	7	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
		CHEMBL205594	76024	7	None	-	1	Human	8.6	pKi	=	8.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	8	2	4	4.2	CCN1CCC(C/N=C(/N)NC(=O)c2cccc(F)c2CCc2cc(Br)ccc2OC)CC1	10.1016/j.bmcl.2006.01.016
		23635107	91558	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		23635107	91558	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		CHEMBL240571	91558	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL240571	91558	0	None	63	3	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	516	9	2	4	4.3	CNCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		23635235	166501	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635235	166501	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL427860	166501	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL427860	166501	0	None	1	5	Human	8.6	pKi	=	8.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		6918850	125422	1	None	154	4	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL364560	125422	1	None	154	4	Human	8.6	pKi	=	8.6	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cellsInhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44400813	71086	0	None	120	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	603	12	4	6	3.9	O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195308	71086	0	None	120	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	603	12	4	6	3.9	O=C(NCCO)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44432963	87452	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233371	87452	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432963	87452	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233371	87452	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	12	0	5	8.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cc4ccccc4s3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL266417	210683	0	None	8	3	Human	7.7	pKi	=	7.7	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm010165y
		CHEMBL3646877	212016	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646877	212016	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88287431	128651	0	None	13	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667923	128651	0	None	13	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3639622	211918	0	None	1	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCN)NC1=O	nan
		88944369	150810	0	None	-1412	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	21	16	11	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3956787	150810	0	None	-1412	2	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	21	16	11	-2.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3577981	211749	1	None	29	3	Mouse	7.7	pKi	=	7.7	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44416298	141892	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	459	7	1	3	5.4	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL386771	141892	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	459	7	1	3	5.4	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		1338	3807	43	None	53	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44432959	87247	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232972	87247	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	544	13	0	5	7.3	CC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44404571	72317	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)CC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198379	72317	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	293	6	0	3	2.5	CCN(CC)CC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		6918857	138709	1	None	33	4	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL377961	138709	1	None	33	4	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		9915636	66824	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL186083	66824	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44433425	88778	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	556	10	1	6	4.3	COCC(COC)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL236319	88778	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	556	10	1	6	4.3	COCC(COC)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44447232	94762	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.9	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL253205	94762	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.9	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412930	138389	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	13	3	7	2.6	CCC(COC)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377258	138389	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	13	3	7	2.6	CCC(COC)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44416209	138940	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.4	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1F	10.1016/j.bmcl.2006.06.075
		CHEMBL378448	138940	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.4	COc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1F	10.1016/j.bmcl.2006.06.075
		44443008	98125	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	585	9	1	5	5.6	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL273565	98125	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	585	9	1	5	5.6	O=C([C@H]1CN(Cc2ccccc2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44404567	72495	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccc(C(F)(F)F)cc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL199003	72495	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccc(C(F)(F)F)cc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44416073	139302	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL379200	139302	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc3ccccc3c2)CC1	10.1016/j.bmcl.2006.06.075
		44434690	89306	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	89306	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434766	154714	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL399810	154714	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	510	9	2	3	6.9	N#Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44347766	114544	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	7	0	3	6.2	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1CC1CC1	10.1016/j.bmcl.2004.05.003
		CHEMBL333702	114544	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	7	0	3	6.2	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1CC1CC1	10.1016/j.bmcl.2004.05.003
		763557	124331	42	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	190	2	0	2	1.4	CN1CCN(Cc2ccccc2)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL363603	124331	42	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	190	2	0	2	1.4	CN1CCN(Cc2ccccc2)CC1	10.1016/j.bmcl.2005.08.018
		44265374	206488	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	454	10	2	2	6.4	O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL8825	206488	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	454	10	2	2	6.4	O=C(O)CCCCCNC(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		168269216	189877	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169353	189877	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168270860	189908	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169826	189908	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5077811	214516	0	None	-36	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/acs.jmedchem.1c00095
		CHEMBL3644283	211927	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644283	211927	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		88944287	152147	0	None	-5128	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	972	16	13	10	-0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)Cc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3968105	152147	0	None	-5128	2	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	972	16	13	10	-0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)Cc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		44433455	147445	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	7	1	4	5.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCC(F)(F)F)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL393010	147445	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	7	1	4	5.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCC(F)(F)F)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44455923	155202	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)ccc2F)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL402510	155202	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)ccc2F)CC1	10.1016/j.bmcl.2007.10.115
		9915636	66824	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL186083	66824	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44410041	141265	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
		CHEMBL383120	141265	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	586	10	2	3	5.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCC2CCCCC2C1	10.1016/j.bmcl.2006.01.016
		44562398	176962	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	550	12	2	5	5.6	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462345	176962	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	550	12	2	5	5.6	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44562459	179020	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	562	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471167	179020	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	562	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		9915636	66824	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186083	66824	0	None	48	4	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	553	12	3	6	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44433448	88484	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL234983	88484	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44433448	88484	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL234983	88484	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	6	1	4	4.9	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44412869	140140	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	559	10	2	6	4.2	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL380222	140140	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	559	10	2	6	4.2	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		16132144	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		16133793	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		44273719	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		CHEMBL214332	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm9017866
		44413930	138648	0	None	1	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL377620	138648	0	None	1	3	Human	7.7	pKi	=	7.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44397199	123633	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	619	11	3	5	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL361882	123633	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	619	11	3	5	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		10408	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		5329	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		9941379	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		CHEMBL2070241	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		DB11653	720	28	None	1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.1c00095
		44323015	111433	0	None	-3	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL327450	111433	0	None	-3	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	731	20	9	8	-0.2	CSCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44396141	66256	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	568	12	3	6	3.2	CC(NCCN1CCCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184623	66256	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	568	12	3	6	3.2	CC(NCCN1CCCCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		11456260	156496	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL406764	156496	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	609	9	3	6	2.5	CS(=O)(=O)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44405365	71946	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197278	71946	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.6	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4N3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44405596	72008	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	11	2	4	4.4	CCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197446	72008	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	11	2	4	4.4	CCCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44415398	80276	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	2	5	5.1	NCCC(=O)NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213953	80276	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	12	2	5	5.1	NCCC(=O)NC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44577055	193296	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL524060	193296	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	447	6	1	3	5.2	CC(C)[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44443002	94487	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.2	CC(C)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251494	94487	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.2	CC(C)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44443000	168890	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	550	8	1	4	4.9	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL438348	168890	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	550	8	1	4	4.9	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44397222	67441	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	620	10	4	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189032	67441	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	620	10	4	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397129	124261	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	621	10	3	5	4.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL363445	124261	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	621	10	3	5	4.3	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44447247	94701	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252824	94701	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44415545	141409	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	3	5.3	Cc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		CHEMBL384040	141409	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	3	5.3	Cc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		44416046	81087	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	473	6	1	5	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cn2cnc3ccccc32)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215531	81087	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	473	6	1	5	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cn2cnc3ccccc32)CC1	10.1016/j.bmcl.2006.06.075
		44434694	88601	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	665	14	3	5	8.7	CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL235589	88601	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	665	14	3	5	8.7	CCOc1cc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		44434706	89597	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237504	89597	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44434855	90030	0	None	-2	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	90030	0	None	-2	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44434870	148148	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL393553	148148	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	NC1CCCC(N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		44434693	167347	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	559	12	2	4	7.4	CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL429451	167347	0	None	1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	559	12	2	4	7.4	CCOc1cc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)ccc1OC	10.1016/j.bmc.2007.06.003
		9842665	156806	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		71461656	79029	7	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	543	6	3	5	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113134	79029	7	None	-	1	Human	5.7	pKi	=	5.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	543	6	3	5	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2NCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		44265496	97049	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL267020	97049	0	None	-4	4	Human	5.7	pKi	=	5.7	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		44434613	89589	0	None	1	2	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	8	2	3	5.1	NCCCN(C(=O)c1cc2cc(OCc3ccccc3)ccc2[nH]1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL237479	89589	0	None	1	2	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	8	2	3	5.1	NCCCN(C(=O)c1cc2cc(OCc3ccccc3)ccc2[nH]1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		44434658	90235	0	None	-2	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL238342	90235	0	None	-2	4	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	10	2	3	3.9	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		44434580	151903	0	None	1	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	335	8	2	2	3.5	NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL396598	151903	0	None	1	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	335	8	2	2	3.5	NCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		11851038	140335	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		168296647	192475	0	None	-33	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5208830	192475	0	None	-33	3	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccccc2CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44409379	76522	0	None	57	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL206018	76522	0	None	57	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	757	19	6	5	4.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(Cl)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		44409337	170461	0	None	39	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		CHEMBL444883	170461	0	None	39	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	721	19	7	6	3.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		89008025	153514	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1069	18	16	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3979831	153514	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1069	18	16	12	-2.2	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644308	211948	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44413600	12298	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	599	8	2	5	4.4	CN1CCC(c2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184893	12298	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	599	8	2	5	4.4	CN1CCC(c2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL376936	12298	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	599	8	2	5	4.4	CN1CCC(c2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44432899	87027	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232533	87027	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL410168	212804	0	None	3	3	Human	7.7	pKi	=	7.7	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		44391304	130453	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	692	13	2	6	5.0	CN(C)CCN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL368022	130453	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	692	13	2	6	5.0	CN(C)CCN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644279	211923	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644279	211923	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		16132144	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44442943	154681	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL399667	154681	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccsc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44397125	67064	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	657	12	3	6	4.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187224	67064	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	657	12	3	6	4.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168293710	192166	0	None	-91	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5203986	192166	0	None	-91	3	Human	7.7	pKi	=	7.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccc(cc3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44322868	106008	0	None	-37	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313279	106008	0	None	-37	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	917	11	12	9	0.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44409140	141286	0	None	10	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		CHEMBL383256	141286	0	None	10	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	675	16	6	5	3.5	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		44395948	123425	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.8	CN(CCc1cccs1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL361714	123425	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.8	CN(CCc1cccs1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		9960253	116949	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL338594	116949	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44433413	88577	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	5	1	4	4.0	CC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235460	88577	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	500	5	1	4	4.0	CC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44444432	94404	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250976	94404	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44432899	87027	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232533	87027	1	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	477	12	2	6	5.5	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCN)cc1	10.1016/j.bmcl.2007.06.010
		44442954	94299	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL250495	94299	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4c[nH]cn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44442972	153018	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397562	153018	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	538	8	1	6	4.2	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cncnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		9960253	116949	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.07.035
		CHEMBL338594	116949	0	None	5	4	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	595	8	3	6	2.8	CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.07.035
		44397279	67135	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3CCCCC3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187521	67135	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3CCCCC3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397196	124068	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	590	10	4	6	2.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C3=CNCC=C3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL363239	124068	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	590	10	4	6	2.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C3=CNCC=C3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44397307	165990	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	10	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL425353	165990	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	587	10	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL2415017	210428	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmc.2013.06.052
		44412711	78172	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL210450	78172	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2006.04.069
		44415546	80238	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccc(C(F)(F)F)c2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213776	80238	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccc(C(F)(F)F)c2)CC1	10.1016/j.bmcl.2006.05.088
		44416007	81080	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	505	9	1	4	5.7	CCOc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL215502	81080	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	505	9	1	4	5.7	CCOc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		44434697	148693	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	543	10	2	4	6.8	COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL393994	148693	0	None	-1	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	543	10	2	4	6.8	COC(=O)c1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44443009	94523	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.7	O=C([C@H]1CNC[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL251699	94523	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.7	O=C([C@H]1CNC[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccncc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		168270860	189908	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5169826	189908	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2812	92	35	37	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44415972	79883	0	None	5	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
		CHEMBL212332	79883	0	None	5	3	Human	6.7	pKi	=	6.7	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	549	13	6	5	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2006.05.087
		44413832	78065	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		CHEMBL210009	78065	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1CCCCN1	10.1021/jm060384p
		44401607	133617	0	None	2	2	Human	6.7	pKi	=	6.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	635	15	6	4	3.7	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL371366	133617	0	None	2	2	Human	6.7	pKi	=	6.7	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	635	15	6	4	3.7	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44432920	87752	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233756	87752	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		44433288	161267	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	11	1	5	4.8	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL412024	161267	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	11	1	5	4.8	CC(C)C[C@H](NC(=O)CN(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400612	69386	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	2	5	5.9	CC(C)CN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL193061	69386	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	2	5	5.9	CC(C)CN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400768	126070	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	650	12	2	6	6.6	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL364913	126070	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	650	12	2	6	6.6	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44562541	172131	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	612	12	3	6	4.4	COc1ccc(CCC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2008.07.076
		CHEMBL447298	172131	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	612	12	3	6	4.4	COc1ccc(CCC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2008.07.076
		88590600	125056	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		CHEMBL3644294	125056	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		88590591	125059	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644305	125059	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644312	211952	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		88590600	125056	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		CHEMBL3644294	125056	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1029	17	16	11	-2.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C(C)C)NC1=O	nan
		88590591	125059	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644305	125059	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2C(N)=O)NC1=O	nan
		CHEMBL3644312	211952	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		44393886	66359	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185145	66359	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	585	9	3	5	4.2	CC(NC1CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44577089	178747	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL468579	178747	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	488	10	2	4	4.5	CNCCN[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		9867330	97841	0	None	100	2	Human	7.6	pKi	=	7.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
		CHEMBL272099	97841	0	None	100	2	Human	7.6	pKi	=	7.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	429	6	1	5	3.7	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCC(Cn2cncn2)(C2CCCCC2)CC1	10.1016/j.bmcl.2007.11.109
		44397027	67439	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	635	11	3	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189004	67439	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	635	11	3	5	4.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44562595	188888	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	549	12	1	5	5.8	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL507347	188888	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	549	12	1	5	5.8	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		11490215	57154	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164671	57154	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	589	10	2	6	3.4	CN(C)CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44405562	72433	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	592	10	2	4	4.8	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198785	72433	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	592	10	2	4	4.8	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3CCCC3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44444450	94106	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	483	8	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNCCN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249168	94106	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	483	8	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNCCN)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44447218	154818	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	654	10	1	5	5.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400379	154818	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	654	10	1	5	5.3	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2C[S+]([O-])C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416227	139243	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		CHEMBL378913	139243	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		71452735	79048	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CO2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113153	79048	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CC(NC2CO2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		44397195	67488	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	593	10	3	6	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189341	67488	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	593	10	3	6	3.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44400824	69839	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	621	12	3	6	5.7	O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL193786	69839	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	621	12	3	6	5.7	O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44415726	78030	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	503	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2csc3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209869	78030	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	503	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2csc3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		44434764	88560	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	551	10	2	2	7.8	NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235358	88560	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	551	10	2	2	7.8	NC1CCC(CC2CCC(N(CCc3c(F)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434653	145815	0	None	-2	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	12	2	2	5.7	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL391706	145815	0	None	-2	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	12	2	2	5.7	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434703	146108	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL391944	146108	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1ccccc1CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434762	153010	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL397550	153010	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	579	11	2	4	7.7	COc1cc(Cl)c(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44432920	87752	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233756	87752	1	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	492	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCO)cc1	10.1016/j.bmcl.2007.06.010
		44434599	89919	0	None	-1	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	333	7	2	2	3.7	NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237957	89919	0	None	-1	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	333	7	2	2	3.7	NCCCN(C/C=C/c1ccccc1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		16132144	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		46885368	7956	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
		CHEMBL1090484	7956	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	6	1	3	4.8	CCCCN1C[C@H](c2ccc(F)cc2F)[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3ccccc3)[C@H](C)C2)C1	10.1021/jm9017866
		168279557	190861	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5184591	190861	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		11845444	80067	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL213026	80067	0	None	-1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		168279557	190861	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5184591	190861	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2996	98	37	39	-8.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44409257	140586	0	None	67	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		CHEMBL381357	140586	0	None	67	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	690	15	7	6	1.6	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.12.005
		44562414	176817	0	None	13	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL460942	176817	0	None	13	3	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44391380	123944	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.6	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)Cc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL362850	123944	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.6	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)Cc3ccccc3C2)CC1	10.1016/j.bmcl.2004.10.096
		11421919	119981	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL349887	119981	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	585	8	2	5	4.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL3646855	211999	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccc(Cl)cc3)CN2C1=O	nan
		134153811	152569	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccc(Cl)cc3)CN2C1=O	nan
		CHEMBL3971788	152569	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccc(Cl)cc3)CN2C1=O	nan
		44393862	123681	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL362147	123681	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	655	11	3	6	5.4	CC(NCCc1cccs1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44393822	124043	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL363074	124043	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	668	9	2	6	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCC(N3CCCC3)CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44577064	187917	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL496710	187917	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	1	4	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44447777	155415	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403675	155415	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443019	154755	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccc(F)c4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400058	154755	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccc(F)c4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		10408	720	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		5329	720	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		9941379	720	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		CHEMBL2070241	720	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		DB11653	720	28	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	10.1021/acs.jmedchem.8b00170
		44433282	88683	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	634	13	2	5	5.6	CC(C)C[C@H](NCCCC(=O)O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL235955	88683	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	634	13	2	5	5.6	CC(C)C[C@H](NCCCC(=O)O)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		71458046	78964	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	2	6	3.2	CN1CCN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113022	78964	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	2	6	3.2	CN1CCN(Cc2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CC1	10.1016/j.bmcl.2004.10.096
		44444457	94147	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	7	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249378	94147	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	7	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN(C)C3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44416208	138929	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1C	10.1016/j.bmcl.2006.06.075
		CHEMBL378425	138929	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1C	10.1016/j.bmcl.2006.06.075
		71458057	79040	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	3	5	3.2	NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113145	79040	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	3	5	3.2	NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44397130	126541	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	665	10	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Br)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365223	126541	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	665	10	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(Br)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		11261324	58134	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL167780	58134	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	547	7	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2[N+](=O)[O-])CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		44415660	80273	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	4	6.7	CCC(C)[C@H](NC(=O)OC)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213935	80273	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	4	6.7	CCC(C)[C@H](NC(=O)OC)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44434692	88525	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	651	13	3	5	8.3	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL235176	88525	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	651	13	3	5	8.3	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434587	89438	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	6	2	3	3.9	NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237094	89438	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	6	2	3	3.9	NCCN(C(=O)[C@H](N)Cc1ccc(Cl)cc1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		44434767	89735	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	616	11	3	4	8.2	N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237689	89735	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	616	11	3	4	8.2	N#Cc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44265315	205932	0	None	-2	2	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	485	15	5	4	4.6	NCCCCNC(=O)[C@H](CCCCNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL8418	205932	0	None	-2	2	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	485	15	5	4	4.6	NCCCCNC(=O)[C@H](CCCCNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		44401592	125190	0	None	4	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	607	13	6	4	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL364519	125190	0	None	4	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	607	13	6	4	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44413536	139929	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL379959	139929	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	753	10	10	7	1.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		168279751	191188	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	66	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5189180	191188	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	66	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168286511	191345	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	70	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5191823	191345	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2905	70	33	37	-5.8	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL50056	214119	2	None	-7	3	Human	6.6	pKi	=	6.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm060384p
		11846844	140079	0	None	-1	3	Human	6.6	pKi	=	6.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL380051	140079	0	None	-1	3	Human	6.6	pKi	=	6.6	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL3646860	212004	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646860	212004	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		44393863	127553	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL366321	127553	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	642	9	4	6	4.4	CC(NC1CCC(N)CC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44415479	81105	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215601	81105	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	586	10	2	4	5.8	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		16046215	80089	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL213122	80089	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		16132144	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16046215	80089	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
		CHEMBL213122	80089	0	None	39	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	441	7	1	3	5.2	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)CC(C)C)c1	10.1021/jm701137s
		44443015	94046	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248862	94046	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4Cl)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL5077095	214479	0	None	-22	3	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL5090946	215285	0	None	-18	3	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL2415086	210437	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCC(=O)NC(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		70693083	76929	0	None	2	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1996	61	24	26	-1.3	CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		91929813	76929	0	None	2	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1996	61	24	26	-1.3	CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		CHEMBL2070253	76929	0	None	2	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL	1996	61	24	26	-1.3	CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44433419	88669	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	6	1	4	4.7	CC(C)C(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235892	88669	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	6	1	4	4.7	CC(C)C(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44456461	157986	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	619	10	1	5	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)c(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL408511	157986	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	619	10	1	5	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)c(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44397131	66785	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL185934	66785	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		44444434	94476	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1cncn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL251380	94476	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1cncn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447212	94603	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	9	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252180	94603	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	610	9	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44397131	66785	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL185934	66785	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		10031074	76343	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
		CHEMBL205898	76343	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	576	13	2	4	6.0	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)NC(C)C	10.1016/j.bmcl.2006.01.016
		44415360	77979	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	541	9	1	5	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)c(OC)c2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209682	77979	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	541	9	1	5	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)c(OC)c2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415791	80404	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(OC)c(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		CHEMBL214537	80404	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(OC)c(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		44416044	80411	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214559	80411	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44416043	80418	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214582	80418	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)c(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434753	89734	0	None	1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	699	12	3	4	9.1	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		CHEMBL237688	89734	0	None	1	3	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	699	12	3	4	9.1	COc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		44434862	90248	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238368	90248	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44348033	16087	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	446	7	0	3	6.7	CCC(C)n1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		CHEMBL122382	16087	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	446	7	0	3	6.7	CCC(C)n1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		71452732	79034	0	None	-3	4	Human	5.6	pKi	=	5.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	697	8	2	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113139	79034	0	None	-3	4	Human	5.6	pKi	=	5.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	697	8	2	6	4.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CN(S(=O)(=O)c2ccccc2)CC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		10225762	145817	0	None	-3	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	448	14	2	3	5.5	CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL391707	145817	0	None	-3	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	448	14	2	3	5.5	CCN(CC)c1ccc(CN(CCCCCN)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		44434858	167251	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL429269	167251	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)N[C@H]2CC[C@H](N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		10025669	97392	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1021/jm020945m
		CHEMBL269776	97392	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1021/jm020945m
		137655905	158828	0	None	-69	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4094606	158828	0	None	-69	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1666	20	22	21	-3.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		56851057	69072	0	None	-1071	3	Human	6.6	pKi	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1069	34	13	10	1.3	C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1021/jm201226w
		CHEMBL1923664	69072	0	None	-1071	3	Human	6.6	pKi	=	6.6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1069	34	13	10	1.3	C#CCCCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCCc1ccccc1)C(N)=O	10.1021/jm201226w
		44401285	135675	0	None	3	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	636	13	5	4	4.1	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL372966	135675	0	None	3	2	Human	6.6	pKi	=	6.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	636	13	5	4	4.1	N=C(N)NCCC[C@H](NC(=O)Cc1ccc(Cl)c(Cl)c1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		16132144	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		168291110	192020	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5201799	192020	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433263	89193	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236732	89193	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416361	141805	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL386259	141805	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		44433291	152791	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397367	152791	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416361	141805	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL386259	141805	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44410046	75951	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
		CHEMBL205214	75951	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	580	10	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN1CCc2ccccc2C1	10.1016/j.bmcl.2006.01.016
		44562599	174262	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.3	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454918	174262	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.3	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44562423	189584	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	9	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL514603	189584	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	9	2	5	3.9	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		44562497	194197	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	10	3	5	3.6	CCCC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL528329	194197	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	10	3	5	3.6	CCCC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44395950	124048	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCNCC1	10.1016/j.bmcl.2004.08.055
		CHEMBL363122	124048	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCNCC1	10.1016/j.bmcl.2004.08.055
		49857745	125064	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644354	125064	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		49857745	125064	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644354	125064	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		16132144	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		16133793	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		44273719	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		CHEMBL214332	209279	36	None	-30	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm201489a
		44434551	89168	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(F)cc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236627	89168	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccc(F)cc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		44433263	89193	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236732	89193	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44433562	88715	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	515	6	1	3	6.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236063	88715	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	515	6	1	3	6.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		44433480	89090	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236527	89090	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	5.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44433384	154710	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL399801	154710	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44433384	154710	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL399801	154710	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	564	7	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44577087	178469	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	4	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL466346	178469	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	461	7	1	4	4.7	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		44416361	141805	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL386259	141805	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	529	7	1	3	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44442931	150390	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL395355	150390	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	536	8	1	4	5.4	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25133207	172943	0	None	16	3	Human	7.6	pKi	=	7.6	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
		CHEMBL451694	172943	0	None	16	3	Human	7.6	pKi	=	7.6	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	11	3	5	2.7	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1(N)CC1	10.1021/jm800525p
		44412512	77941	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	629	11	3	6	3.4	CS(=O)(=O)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209559	77941	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	629	11	3	6	3.4	CS(=O)(=O)NCC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		10257541	126342	0	None	123	4	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL365039	126342	0	None	123	4	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@@H]2CCCC[C@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44433418	88625	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	7	1	4	4.8	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235676	88625	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	528	7	1	4	4.8	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44455892	97919	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL272515	97919	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	617	10	1	5	5.2	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		44433387	151961	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	598	7	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL396657	151961	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	598	7	1	4	7.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44405375	140352	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
		CHEMBL380769	140352	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	655	10	3	5	4.4	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc21	10.1016/j.bmcl.2005.08.061
		44447228	154613	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	6	1	5	5.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL399241	154613	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	6	1	5	5.0	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		11851038	140335	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		24740311	89251	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236802	89251	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44397053	67435	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	660	11	4	7	3.8	COC(=O)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL188980	67435	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	660	11	4	7	3.8	COC(=O)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44396957	67959	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	577	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccco3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL191159	67959	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	577	10	3	6	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccco3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		10255546	77331	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	503	8	2	2	5.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCC1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL208367	77331	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	503	8	2	2	5.4	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCC1CCCCC1	10.1016/j.bmcl.2006.01.016
		156015336	177519	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	3793	77	53	60	-15.9	CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2	10.1021/acs.jmedchem.0c00485
		CHEMBL4639782	177519	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	3793	77	53	60	-15.9	CC[C@H](C)[C@@H]1NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]2CSSC[C@@H](C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](N)CCC(N)=O)CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)CNC1=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N3)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2	10.1021/acs.jmedchem.0c00485
		44412729	77437	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	3	7	2.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccco2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208679	77437	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	3	7	2.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)c2ccco2)CC1	10.1016/j.bmcl.2006.04.069
		44415764	81118	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c(Cl)cccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215646	81118	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c(Cl)cccc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415337	141668	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	619	11	1	3	8.2	CCC(C)[C@H](NCCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL385437	141668	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	619	11	1	3	8.2	CCC(C)[C@H](NCCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44416072	80098	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc3ccccc23)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213153	80098	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	499	7	1	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc3ccccc23)CC1	10.1016/j.bmcl.2006.06.075
		44416126	80920	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215332	80920	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434781	89904	0	None	-6	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237919	89904	0	None	-6	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434768	154715	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	9	2	2	8.3	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL399811	154715	0	None	-1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	9	2	2	8.3	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		70690147	75083	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	474	10	2	4	2.7	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035945	75083	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	474	10	2	4	2.7	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		70684954	77819	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL2092821	77819	0	None	-2	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		44410349	76192	0	None	-	1	Human	4.6	pKi	=	4.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	460	11	2	3	4.8	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccccc1Cl	10.1016/j.bmcl.2006.01.016
		CHEMBL205813	76192	0	None	-	1	Human	4.6	pKi	=	4.6	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	460	11	2	3	4.8	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccccc1Cl	10.1016/j.bmcl.2006.01.016
		10291369	168922	0	None	-4	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	8	2	2	3.6	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL438672	168922	0	None	-4	3	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	8	2	2	3.6	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44416122	80128	0	None	1	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL213284	80128	0	None	1	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	576	11	4	5	1.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		44404542	72375	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	323	5	0	4	2.2	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(=O)OC	10.1016/j.bmcl.2005.08.018
		CHEMBL198606	72375	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	323	5	0	4	2.2	CCN(CC(c1ccccc1F)N1CCN(C)CC1)C(=O)OC	10.1016/j.bmcl.2005.08.018
		168291110	192020	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5201799	192020	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3073	99	37	39	-7.7	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168271237	190488	0	None	-93	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5179081	190488	0	None	-93	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2788	45	36	36	0.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		46885323	8209	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092209	8209	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	414	3	2	3	3.3	C[C@H]1CN(C(=O)[C@@H]2CNC[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44433279	151709	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396433	151709	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	656	11	2	5	5.7	CC(C)C[C@H](NCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11330869	119980	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL349886	119980	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	599	8	2	5	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		44394079	126765	0	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL365278	126765	0	None	1	4	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccccc2F)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44577088	189409	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	6	1	3	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL513128	189409	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	6	1	3	5.3	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2008.03.072
		44443029	93697	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	582	9	1	5	6.1	CSc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL247009	93697	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	582	9	1	5	6.1	CSc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44442981	153078	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397608	153078	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11328898	7960	22	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1090488	7960	22	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1204059	7960	22	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	470	3	1	3	4.8	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		24886498	12290	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	643	10	2	6	3.6	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(S(C)(=O)=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184873	12290	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	643	10	2	6	3.6	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(S(C)(=O)=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL375388	12290	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	643	10	2	6	3.6	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(S(C)(=O)=O)CC1	10.1016/j.bmcl.2006.04.016
		168285465	191632	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5195766	191632	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		24848995	117947	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		CHEMBL340355	117947	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2008.07.076
		44391286	122617	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	656	12	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCC2=O)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL360296	122617	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	656	12	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCN2CCCC2=O)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		24848995	117947	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL340355	117947	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44405561	71941	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	11	2	4	4.6	CC(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197272	71941	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	580	11	2	4	4.6	CC(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44444452	154093	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	497	9	2	5	3.4	CNCCNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL398489	154093	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	497	9	2	5	3.4	CNCCNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		24848995	117947	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		CHEMBL340355	117947	0	None	-11	3	Human	6.6	pKi	=	6.6	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Cn2cncn2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm049278i
		44348069	15688	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)cn1C	10.1016/j.bmcl.2004.05.003
		CHEMBL122236	15688	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	384	5	0	3	5.0	COc1ccc(Br)cc1CCc1ccccc1-c1nc(C)cn1C	10.1016/j.bmcl.2004.05.003
		44396954	66845	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	10	3	5	4.0	Cc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL186188	66845	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	10	3	5	4.0	Cc1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44434698	171025	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	3	5	8.1	COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL445669	171025	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	3	5	8.1	COC(=O)c1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44443043	154660	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	10	0	5	6.2	CC(C)CN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL399570	154660	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	10	0	5	6.2	CC(C)CN(Cc1ccncc1)CC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		9968756	89509	0	None	-16	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	5	1	2	3.7	NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL237299	89509	0	None	-16	4	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	5	1	2	3.7	NCCN(C(=O)Cc1ccc2ccccc2c1)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		10025669	97392	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL269776	97392	0	None	-39	4	Human	4.6	pKi	=	4.6	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	429	11	5	4	3.0	NCCCNC(=O)[C@H](CNCc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		11851038	140335	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44401341	135673	0	None	3	2	Human	5.6	pKi	=	5.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	630	13	5	4	4.5	N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL372965	135673	0	None	3	2	Human	5.6	pKi	=	5.6	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	630	13	5	4	4.5	N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562597	189052	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL509475	189052	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3646886	212024	0	None	29	2	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646886	212024	0	None	29	2	Human	7.6	pKi	=	7.6	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44447242	94982	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254701	94982	0	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44432965	145759	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL391665	145759	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432965	145759	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL391665	145759	1	None	-	1	Human	7.6	pKi	=	7.6	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	546	14	0	5	7.0	COc1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44562560	174253	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	463	7	2	4	4.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454905	174253	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	463	7	2	4	4.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL50056	214119	2	None	-7	3	Human	6.6	pKi	=	6.6	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44405392	72452	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	2	5	4.8	CC(C)COC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198851	72452	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	2	5	4.8	CC(C)COC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44447226	94723	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252993	94723	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44444433	154389	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL398756	154389	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	505	6	0	5	4.7	Cc1nccn1Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447233	154887	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	489	6	1	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400783	154887	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	489	6	1	4	5.5	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447208	155288	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	539	6	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL402917	155288	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	539	6	1	4	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CSC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		71456251	79035	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	2	5	3.4	CN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113140	79035	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	571	6	2	5	3.4	CN1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44412770	78502	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	520	9	3	6	1.7	CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211187	78502	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	520	9	3	6	1.7	CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44415369	79604	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2F)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL211462	79604	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2F)CC1	10.1016/j.bmcl.2006.05.088
		44415691	80151	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	585	11	1	3	8.0	CCC(C)CN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		CHEMBL213389	80151	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	585	11	1	3	8.0	CCC(C)CN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		44416020	139112	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL378671	139112	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44434760	88517	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	519	9	2	2	7.6	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235140	88517	0	None	1	4	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	519	9	2	2	7.6	NC1CCC(CC2CCC(N(Cc3ccccc3Cl)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44443039	154659	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	686	12	0	6	7.3	COc1ccc(CN(Cc2ccc(OC)cc2)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL399564	154659	0	None	-	1	Human	5.6	pKi	=	5.6	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	686	12	0	6	7.3	COc1ccc(CN(Cc2ccc(OC)cc2)CC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		88944284	148526	0	None	-9549	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	986	17	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CCc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3938542	148526	0	None	-9549	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	986	17	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CCc2ccccc2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		11845804	79558	0	None	-616	3	Human	5.5	pKi	=	5.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL211419	79558	0	None	-616	3	Human	5.5	pKi	=	5.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		168287469	191521	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5194073	191521	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44562518	186758	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	3	5	3.6	C=CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488884	186758	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	3	5	3.6	C=CC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44413876	79744	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		CHEMBL211699	79744	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1016/j.bmcl.2006.05.087
		168285465	191632	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5195766	191632	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2721	92	33	35	-6.2	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL4211294	213265	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK cell membranes after 1 hr by liquid scintillation countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK cell membranes after 1 hr by liquid scintillation counting	ChEMBL		None	None	None		CC(C)C[C@@H]1NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](C(C)C)NC(=O)[C@@H]5CCCN5C1=O)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N4)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC3=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N2	10.1021/acs.jmedchem.8b00378
		44434556	145157	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL391219	145157	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	601	10	3	5	4.8	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL438596	213781	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44442998	93606	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL246631	93606	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	578	8	1	5	5.2	O=C([C@H]1CN(C2CCOCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		44443026	154802	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL400263	154802	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	5.4	CC(=O)Nc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44413876	79744	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
		CHEMBL211699	79744	0	None	-2	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	710	18	8	7	0.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O	10.1021/jm060384p
		11308054	133616	0	None	8	2	Human	7.5	pKi	=	7.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL371365	133616	0	None	8	2	Human	7.5	pKi	=	7.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	618	13	5	4	3.9	N=C(N)NCCC[C@H](NC(=O)Cc1cccc2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562422	179065	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471517	179065	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44395513	66202	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	7	3.9	NCCC(=O)OC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184424	66202	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	7	3.9	NCCC(=O)OC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44396068	127548	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	626	13	4	6	5.0	CC(NCCNc1cccc2ccccc12)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL366303	127548	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	626	13	4	6	5.0	CC(NCCNc1cccc2ccccc12)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44455891	97918	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL272514	97918	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44447229	154948	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	636	10	1	6	5.1	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL401110	154948	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	636	10	1	6	5.1	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2C(=O)OCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		46885367	7852	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089797	7852	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	454	4	1	3	4.1	C[C@H]1CN(C(=O)[C@H]2CN(C3CC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44397216	126832	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	483	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CN)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365491	126832	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	483	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CN)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44416071	80097	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213152	80097	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		1016	3747	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2561	3747	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		2733526	3747	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		5384	3747	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		CHEMBL83	3747	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		DB00675	3747	78	None	-70	35	Human	4.5	pKi	=	4.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
		53236833	146568	0	None	-4168	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1024	19	14	11	-1.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3922906	146568	0	None	-4168	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1024	19	14	11	-1.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		168277258	190710	0	None	-5	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5182345	190710	0	None	-5	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1243	15	14	15	-0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL3644285	211929	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644285	211929	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		9842665	156806	12	None	-3	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		88212371	144161	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1039	18	15	12	-2.1	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3904001	144161	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1039	18	15	12	-2.1	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644295	211938	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3644361	211994	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88590619	125525	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646852	125525	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		117723617	160392	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	16	16	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL4111210	160392	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	16	16	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3644296	211939	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644309	211949	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3644323	211963	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644347	211986	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		88590619	125525	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646852	125525	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1070	19	17	12	-2.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		134137220	142902	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		CHEMBL3893727	142902	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		134133748	143170	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		CHEMBL3896045	143170	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1117	18	15	11	3.2	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3)CN2C1=O	nan
		134153479	152812	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1134	19	15	12	3.6	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		CHEMBL3973826	152812	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1134	19	15	12	3.6	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](OCc3ccccc3)CN2C1=O	nan
		90684345	160096	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1040	18	15	11	-2.8	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL4108637	160096	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1040	18	15	11	-2.8	CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C[n+]2cc[nH]c2)NC1=O	nan
		CHEMBL3644296	211939	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644323	211963	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644361	211994	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646876	212015	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3663317	212049	0	None	-3	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663354	212084	0	None	95	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663357	212087	0	None	1412	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3663379	212108	0	None	17	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3667916	212113	0	None	50	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667917	212114	0	None	56	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667922	212118	0	None	63	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667933	212127	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		COc1cccc(C[C@H]2NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC2=O)c1	nan
		CHEMBL3667941	212135	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)c(F)c(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88944398	152955	0	None	-301	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3975096	152955	0	None	-301	2	Human	8.5	pKi	=	8.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1021	19	13	11	-0.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		1338	3807	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
		9938402	3807	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
		CHEMBL339053	3807	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2007.11.109
		44412574	78055	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209990	78055	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44412612	138925	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL378408	138925	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		44412513	159414	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL410087	159414	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		44400661	124339	0	None	512	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	620	11	2	5	6.1	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL363641	124339	0	None	512	2	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	620	11	2	5	6.1	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL2415082	210433	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		44577061	192641	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL521715	192641	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	9	2	5	4.0	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2c(F)cccc2[C@@H](NC(=O)C2CNC2)C(C)C)CC1	10.1016/j.bmc.2008.03.072
		44347840	161924	0	None	17	3	Human	8.5	pKi	=	8.5	Binding	Inhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determined	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		91932630	161924	0	None	17	3	Human	8.5	pKi	=	8.5	Binding	Inhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determined	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		CHEMBL415333	161924	0	None	17	3	Human	8.5	pKi	=	8.5	Binding	Inhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determinedInhibitory activity against human melanocortin receptor human Melanocortin 4 receptor was determined	ChEMBL	1590	33	17	23	-2.2	CC(=O)[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)CN2CCC[C@H]2C(=O)CN[C@@H](CCCCN)C(=O)CN[C@@H](CC(=O)O)C(N)=O)NC(=O)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm030111j
		24740535	89349	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	544	8	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2007.07.097
		CHEMBL236939	89349	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	544	8	1	4	5.2	Cc1ccc(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)N3CCCC3=O)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2007.07.097
		23635235	166501	0	None	-1	5	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		CHEMBL427860	166501	0	None	-1	5	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	526	10	1	4	4.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1021/jm070806a
		6918844	168622	1	None	173	4	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF	10.1016/j.bmcl.2005.03.053
		CHEMBL436122	168622	1	None	173	4	Human	8.5	pKi	=	8.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	6	5.3	O=C(N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCCF	10.1016/j.bmcl.2005.03.053
		10369375	77218	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL207946	77218	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	518	9	2	3	4.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCCCC1	10.1016/j.bmcl.2006.01.016
		44562460	189265	0	None	165	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL511826	189265	0	None	165	3	Human	8.5	pKi	=	8.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	10	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		1338	3807	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL267492	210724	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44432962	145758	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL391664	145758	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432962	145758	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL391664	145758	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	555	12	0	5	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3cn(C)c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44434553	89294	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236839	89294	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		44434559	89493	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237267	89493	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		44577094	178647	0	None	117	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL467588	178647	0	None	117	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	546	10	1	4	5.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44432932	87754	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233758	87754	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432932	87754	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233758	87754	0	None	38	4	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	6.6	CNC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL2415084	210435	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc2cn(CCCCCC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N3CCC[C@H]3C(=O)N[C@H](C(N)=O)C(C)C)nn2)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		44577091	178667	0	None	19	3	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL467772	178667	0	None	19	3	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	532	10	2	5	4.0	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2OC)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		24180592	97013	0	None	5	6	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		CHEMBL266647	97013	0	None	5	6	Human	8.5	pKi	=	8.5	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	560	11	1	4	5.7	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1021/jm701137s
		44577060	188052	0	None	1	8	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL497746	188052	0	None	1	8	Mouse	8.5	pKi	=	8.5	Binding	Binding affinity at mouse MC4RBinding affinity at mouse MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44443023	155019	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL401487	155019	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44432939	87244	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232951	87244	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		24740653	88592	0	None	190	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		CHEMBL235556	88592	0	None	190	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	11	1	4	5.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@H](CC(C)C)NC(=O)CCN(C)C)c1	10.1021/jm701137s
		44432939	87244	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232951	87244	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	2	6	7.1	CC(=O)Nc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44433284	88570	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	10	2	5	4.2	CC(C)C[C@H](NC(=O)CN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL235421	88570	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	10	2	5	4.2	CC(C)C[C@H](NC(=O)CN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433272	147712	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL393204	147712	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	587	12	2	5	4.8	CNCCN[C@@H](CC(C)C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44432964	87453	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233372	87453	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44432964	87453	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233372	87453	0	None	1148	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	558	14	0	5	7.2	CC(=O)c1ccc(Cc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44391405	66085	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	587	10	3	5	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183831	66085	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	587	10	3	5	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		44395615	66165	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	595	13	3	6	4.5	CC(C)CC(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184272	66165	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	595	13	3	6	4.5	CC(C)CC(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644291	211935	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		88590641	125061	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		CHEMBL3644307	125061	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		117723615	149971	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1066	19	16	12	-1.3	N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		CHEMBL3949958	149971	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1066	19	16	12	-1.3	N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		CHEMBL3644280	211924	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		88590641	125061	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		CHEMBL3644307	125061	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1120	19	17	12	-2.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(C(N)=O)cc2)NC1=O	nan
		CHEMBL3644280	211924	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644291	211935	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646864	212007	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](COCc2ccccc2)NC1=O	nan
		CHEMBL3663382	212111	0	None	25	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		166585440	191918	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		CHEMBL5200190	191918	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	463	4	1	10	1.8	COc1cc([C@H](C)C(=O)N2CC[C@@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)nc(C)n1	10.1021/acsmedchemlett.2c00229
		44433381	88665	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	626	7	1	4	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235852	88665	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	626	7	1	4	6.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)c3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415707	141529	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	11	2	4	6.3	CCC(C)[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384636	141529	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	11	2	4	6.3	CCC(C)[C@H](NCCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447241	154683	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL399677	154683	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2COC[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44443020	94089	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL249065	94089	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1cccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)c1	10.1016/j.bmcl.2007.10.032
		CHEMBL5087814	215119	0	None	-8	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL5087859	215123	0	None	-436	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		10283067	76527	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL206042	76527	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL410672	212830	0	None	4	2	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		168277916	190677	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4986	94	68	63	-6.6	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5181812	190677	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4986	94	68	63	-6.6	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		168284256	190946	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5185775	190946	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2383	48	33	31	-4.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC/C(=N/OCC(=O)NCCOCCOCCOCCN=[N+]=[N-])CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432957	87208	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232774	87208	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		44415377	80322	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	11	2	5	4.0	CCOCC(NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL214204	80322	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	11	2	5	4.0	CCOCC(NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44405620	134290	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	2	4	4.2	CC(C)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL371703	134290	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	566	10	2	4	4.2	CC(C)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		9842665	156806	12	None	-3	2	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44442914	145114	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	4	5.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCC4CCCCC4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL391183	145114	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	4	5.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCC4CCCCC4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		46885560	7811	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089485	7811	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ncccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44347976	16437	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	404	5	0	3	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C	10.1016/j.bmcl.2004.05.003
		CHEMBL123258	16437	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	404	5	0	3	5.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C	10.1016/j.bmcl.2004.05.003
		44415748	141482	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cn(C)c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384390	141482	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	500	7	1	4	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cn(C)c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		44434770	88561	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	521	9	2	2	7.3	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235359	88561	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	521	9	2	2	7.3	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434701	89501	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		CHEMBL237291	89501	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	499	9	2	2	7.3	Cc1cccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		44434771	148790	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	627	11	3	3	8.6	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL394073	148790	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	627	11	3	3	8.6	NC1CCC(CC2CCC(N(Cc3c(F)cccc3F)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44443010	94003	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	7	1	5	3.9	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248669	94003	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	7	1	5	3.9	CC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44265751	106098	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL313379	106098	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		44393441	66429	0	None	-2	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL185195	66429	0	None	-2	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL3644286	211930	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644286	211930	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		168278271	191115	0	None	-30	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5187932	191115	0	None	-30	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2167	35	34	26	-5.3	CCCC[C@@H]1NC(=O)[C@@H]2CS/C(C(=O)O)=C(/C(N)=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		11851038	140335	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		11845813	139804	0	None	1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		CHEMBL379879	139804	0	None	1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	10	3	4	3.0	NC(N)=NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@H](N)Cc1ccccc1	10.1021/jm060384p
		CHEMBL5091245	215300	0	None	-7	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137653925	158607	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4092141	158607	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44415966	166101	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL425962	166101	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44400709	168596	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	5	6.4	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1ccccc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL435933	168596	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	606	12	2	5	6.4	O=C([C@@H](Cc1ccc(Cl)cc1Cl)NCc1ccccc1)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44415966	166101	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL425962	166101	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44562422	179065	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471517	179065	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	532	10	2	5	3.8	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44433417	148360	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	4.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL393726	148360	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	4	4.4	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44416349	81109	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215617	81109	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44415966	166101	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL425962	166101	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44432957	87208	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232774	87208	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	526	15	2	6	5.0	CC(=O)NCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		11846669	80277	0	None	1	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		CHEMBL213956	80277	0	None	1	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	584	12	5	5	3.5	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCCN1	10.1021/jm060384p
		24886734	11827	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	566	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCOCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182130	11827	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	566	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCOCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL213940	11827	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	566	9	2	5	4.3	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCOCC1	10.1016/j.bmcl.2006.04.016
		44413002	172553	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	11	3	7	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL448475	172553	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	602	11	3	7	3.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		44442903	145903	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	1	5	4.2	COCC(C)NCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL391780	145903	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	1	5	4.2	COCC(C)NCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		44347977	168291	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	418	6	0	3	5.8	CCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		CHEMBL434029	168291	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	418	6	0	3	5.8	CCn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2004.05.003
		44401581	68630	0	None	2	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL191794	68630	0	None	2	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	602	13	5	4	3.4	N=C(N)NCCC[C@H](NC(=O)Cc1ccccc1Cl)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44416109	80908	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	494	8	1	6	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215290	80908	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	494	8	1	6	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc([N+](=O)[O-])cc2)CC1	10.1016/j.bmcl.2006.06.075
		44416006	141561	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL384852	141561	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.3	COc1cccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.06.075
		44434854	90029	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238153	90029	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		11851038	140335	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		44443011	154009	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	1	5	4.3	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398408	154009	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	1	5	4.3	CCC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		46905544	10299	0	None	-4	2	Human	4.5	pKi	=	4.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	641	14	6	5	2.6	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL1161791	10299	0	None	-4	2	Human	4.5	pKi	=	4.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	641	14	6	5	2.6	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44265751	106098	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1021/jm020945m
		CHEMBL313379	106098	0	None	-7	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	412	12	7	4	0.3	N=C(N)NCCCNC(=O)[C@H](CCCN=C(N)N)NCc1ccc2ccccc2c1	10.1021/jm020945m
		CHEMBL1201469	14507	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		None	nan
		44413535	96705	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL264120	96705	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	738	10	9	7	2.9	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC[C@H](Cc2c[nH]cn2)NC(=O)CCCCCCCC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		44562540	188962	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	582	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CCc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508293	188962	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	582	11	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CCc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644298	211941	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3644298	211941	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44433479	89089	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236526	89089	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		16132144	209279	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44443028	94125	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	9	1	6	5.2	COC(=O)c1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		CHEMBL249270	94125	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	594	9	1	6	5.2	COC(=O)c1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1	10.1016/j.bmcl.2007.10.032
		44432913	87382	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233336	87382	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL3577976	211744	0	None	2	2	Mouse	6.5	pKi	=	6.5	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		44444436	94372	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cncn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250797	94372	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cncn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44444443	161772	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	9	0	5	4.2	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL413989	161772	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	9	0	5	4.2	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44348152	16433	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	414	5	0	3	5.2	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL123215	16433	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	414	5	0	3	5.2	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCC2	10.1016/j.bmcl.2004.05.003
		44348070	113925	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cnc(-c2ccccc2CCc2cc(Br)ccc2OC)n1C	10.1016/j.bmcl.2004.05.003
		CHEMBL332584	113925	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cnc(-c2ccccc2CCc2cc(Br)ccc2OC)n1C	10.1016/j.bmcl.2004.05.003
		44562389	176136	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	603	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL459218	176136	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	603	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44434772	88597	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	88597	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434855	90030	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	90030	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44434860	90042	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238159	90042	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	449	8	2	2	5.9	N[C@H]1CC[C@H](N(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44434757	152741	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	2	4	8.3	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL397324	152741	0	None	-1	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	649	12	2	4	8.3	COc1cc(Br)c(/C=C/CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434598	89816	0	None	-6	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.5	NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237743	89816	0	None	-6	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	349	9	2	2	3.5	NCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		88944288	149904	0	None	-12882	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3949338	149904	0	None	-12882	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44412572	139013	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	632	11	2	4	7.2	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL378568	139013	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	632	11	2	4	7.2	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(CC2CCCCC2)CC2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		44562421	179064	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	518	9	2	5	3.6	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471516	179064	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	518	9	2	5	3.6	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		44391404	123134	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	11	3	5	4.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL361210	123134	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	11	3	5	4.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644290	211934	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O	nan
		117723603	147081	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1072	19	17	12	-3.4	CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3927218	147081	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1072	19	17	12	-3.4	CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644290	211934	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O	nan
		CHEMBL3644341	211981	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3663322	212054	0	None	1	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C#N)c2)NC(=O)[C@H](CCN)NC1=O	nan
		88944296	142595	0	None	-60	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3891338	142595	0	None	-60	2	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1010	19	14	11	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL2415080	210431	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		1338	3807	43	None	53	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
		9938402	3807	43	None	53	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
		CHEMBL339053	3807	43	None	53	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2004.06.059
		44393889	66347	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185094	66347	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	667	11	3	5	5.5	CC(NCCc1ccccc1F)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44432954	87045	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232585	87045	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432913	87382	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233336	87382	1	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	561	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCOCC2)cc1	10.1016/j.bmcl.2007.06.010
		168273645	190325	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	5162	106	68	67	-6.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5176443	190325	0	None	-79	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	5162	106	68	67	-6.5	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		168289457	191380	0	None	-20	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5192329	191380	0	None	-20	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3ccccc3CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432954	87045	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232585	87045	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	523	13	1	6	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccsc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		168289404	191312	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5191309	191312	0	None	-46	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2134	33	32	28	-5.0	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(nn3)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44562363	176971	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	551	12	2	5	5.7	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462379	176971	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	551	12	2	5	5.7	CSCCCN[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL2415085	210436	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCCCC(CCCNC(C)=O)(NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		44447231	154907	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400882	154907	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447809	95326	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	480	5	1	4	3.8	CC(=O)N1CC[C@H](c2ccc(F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256540	95326	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	480	5	1	4	3.8	CC(=O)N1CC[C@H](c2ccc(F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44442902	145634	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	586	8	1	5	4.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)c4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL391570	145634	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	586	8	1	5	4.6	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)c4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44415384	141580	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	463	7	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2O)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384965	141580	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	463	7	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccccc2O)CC1	10.1016/j.bmcl.2006.05.088
		44434772	88597	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	88597	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434849	146856	0	None	-17	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	411	9	2	2	5.2	NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		CHEMBL392521	146856	0	None	-17	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	411	9	2	2	5.2	NCc1cccc(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		10292084	148395	0	None	-13	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	6	2	2	3.4	NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL393755	148395	0	None	-13	4	Human	4.5	pKi	=	4.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	6	2	2	3.4	NCCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		44401513	69162	0	None	-1	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	612	13	5	6	2.5	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL192450	69162	0	None	-1	2	Human	6.5	pKi	=	6.5	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	612	13	5	6	2.5	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2c(c1)OCO2)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		168287469	191521	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5194073	191521	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2959	96	36	38	-8.0	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44391403	65270	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	602	10	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)c2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL182823	65270	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	602	10	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)c2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		11157584	168244	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL433710	168244	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		88565601	125063	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644353	125063	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		88565601	125063	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644353	125063	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1086	20	17	12	-3.0	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		11249788	120114	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL351088	120114	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44433483	145764	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL391667	145764	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44447765	155074	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NC(=O)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401797	155074	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NC(=O)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44442901	93739	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	600	9	1	5	4.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247230	93739	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	600	9	1	5	4.7	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNS(=O)(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		10411266	114330	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	5	0	3	6.1	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL333075	114330	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	444	5	0	3	6.1	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		44397080	67165	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	567	11	3	5	4.2	CC(C)(C)CCNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187657	67165	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	567	11	3	5	4.2	CC(C)(C)CCNCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		44396955	168225	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	655	10	3	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL433598	168225	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	655	10	3	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44434843	88700	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236020	88700	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	89743	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434684	146599	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	12	2	2	5.0	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL392315	146599	0	None	1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	391	12	2	2	5.0	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434845	147903	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	527	10	4	2	6.5	N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393350	147903	0	None	-2	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	527	10	4	2	6.5	N=C(N)NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434702	149513	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		CHEMBL394646	149513	0	None	-1	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1cccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)c1	10.1016/j.bmc.2007.06.003
		44443013	94045	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	6	3.3	CS(=O)(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248861	94045	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	573	8	1	6	3.3	CS(=O)(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44412559	155738	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	539	10	2	5	3.0	CCN(CC)CC(C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL405601	155738	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	539	10	2	5	3.0	CCN(CC)CC(C)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		46885863	8472	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		CHEMBL1093858	8472	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	446	3	1	3	3.8	C[C@H]1CN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		168290510	191897	0	None	-1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5199932	191897	0	None	-1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1215	15	14	15	-1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5085972	215003	0	None	-1	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.1c00095
		11330992	119934	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL349515	119934	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	615	12	2	5	5.1	CCCN(CCC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL3644303	211946	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CSCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646859	212003	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646861	212005	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644303	211946	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CSCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646861	212005	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646866	212009	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663341	212071	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		COc1ccc(C[C@H]2NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC2=O)cc1OC	nan
		CHEMBL2070254	209185	0	None	7	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44393821	66712	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185583	66712	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	650	11	2	6	4.5	CN(CCc1ccccn1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		23634985	154829	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23634985	154829	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		CHEMBL400412	154829	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL400412	154829	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	445	6	1	3	5.0	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3F)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		44442978	153076	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397607	153076	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccnc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25132867	172498	0	None	6	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
		CHEMBL448337	172498	0	None	6	3	Human	7.5	pKi	=	7.5	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccccn1	10.1021/jm800525p
		44412647	78396	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	604	9	2	4	6.5	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(C2CCCCC2)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL211078	78396	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	604	9	2	4	6.5	O=C(CC1Cc2ccccc2N1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C(C2CCCCC2)C2CCCCC2)CC1	10.1016/j.bmcl.2006.04.002
		168276507	190265	0	None	-87	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5175487	190265	0	None	-87	3	Human	7.5	pKi	=	7.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2158	33	32	24	-2.3	CCCC[C@@H]1NC(=O)[C@@H]2CSCc3cccc(c3)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44562412	175099	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	602	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL456886	175099	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	602	16	1	4	8.0	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44562401	189705	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	570	12	1	4	6.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC2CC2)CC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL515512	189705	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	570	12	1	4	6.4	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(CC2CC2)CC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		44322994	106997	0	None	-3	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL315258	106997	0	None	-3	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	715	20	9	8	-1.0	COCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		11341811	120124	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL351161	120124	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	7	3	5	3.5	C[C@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		46930943	68405	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		CHEMBL1917059	68405	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44433421	146276	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	568	6	1	4	5.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL392069	146276	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	568	6	1	4	5.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415361	80070	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.05.088
		CHEMBL213041	80070	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.05.088
		46885815	7860	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		CHEMBL1089830	7860	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	471	3	1	4	4.2	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		44397132	127302	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccccc1C(=O)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		CHEMBL365893	127302	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	617	11	3	6	3.7	COc1ccccc1C(=O)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)CCCCC1	10.1016/j.bmcl.2005.05.017
		44434778	89743	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL5092761	215388	0	None	-501	3	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
		46885907	8040	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		CHEMBL1090885	8040	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	460	4	1	3	4.1	CCN1C[C@@H](C(=O)N2C[C@H](C)[C@@](O)(c3cccc(F)c3)[C@H](C)C2)[C@H](c2ccc(F)cc2F)C1	10.1021/jm9017866
		88944400	153291	0	None	-8912	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3977876	153291	0	None	-8912	2	Human	6.5	pKi	=	6.5	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.8	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44391288	65951	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	608	9	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNc2ccncc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL183610	65951	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	608	9	3	6	4.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNc2ccncc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44433441	89925	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	544	7	1	4	5.9	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(Cc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL237977	89925	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	544	7	1	4	5.9	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(Cc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44397224	67321	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL188432	67321	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		44416182	80168	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	511	7	2	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2O)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213469	80168	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	511	7	2	4	5.6	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2O)CC1	10.1016/j.bmcl.2006.06.075
		24741961	89365	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	462	7	1	4	5.0	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236978	89365	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	462	7	1	4	5.0	CC(C)C[C@@H](N)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		46885712	8071	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		CHEMBL1091151	8071	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		CHEMBL1204061	8071	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(F)cc1	10.1021/jm9017866
		46885417	8281	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092573	8281	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	498	4	1	4	4.2	C[C@H]1CN(C(=O)[C@H]2CN(C3CCOCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		25128751	173584	0	None	11	3	Human	7.4	pKi	=	7.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
		CHEMBL453300	173584	0	None	11	3	Human	7.4	pKi	=	7.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	2	6	4.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cscn1	10.1021/jm800525p
		44397224	67321	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL188432	67321	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	632	11	4	6	4.0	COc1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44397306	67464	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	576	11	4	6	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3=CC=CCN3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL189172	67464	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	576	11	4	6	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCC3=CC=CCN3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL5080784	214706	0	None	-9	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44412679	78828	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccccc1CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211279	78828	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccccc1CC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44415675	79876	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	557	8	1	3	6.5	CCC(C)[C@H](NC(C)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212303	79876	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	557	8	1	3	6.5	CCC(C)[C@H](NC(C)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444446	154876	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	6	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400712	154876	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	509	6	1	5	3.5	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCNCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44400902	71006	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	3	7	4.0	O=C(N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL195172	71006	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	572	12	3	7	4.0	O=C(N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44416045	80412	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	448	7	2	4	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CNc2ccccc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214560	80412	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	448	7	2	4	4.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CNc2ccccc2)CC1	10.1016/j.bmcl.2006.06.075
		44434884	88611	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235617	88611	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		70682904	77866	0	None	1	2	Human	4.4	pKi	=	4.4	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL2093089	77866	0	None	1	2	Human	4.4	pKi	=	4.4	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	383	5	2	2	4.6	O=C(NCc1c[nH]c2ccccc12)[C@H]1CCCN1Cc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		70660687	144910	0	None	-912	2	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	800	16	12	10	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3910197	144910	0	None	-912	2	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	800	16	12	10	-2.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		44416014	80015	0	None	16	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL212855	80015	0	None	16	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	562	10	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNC(N)=O)C1=O	10.1016/j.bmcl.2006.05.087
		88590646	125530	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646883	125530	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590646	125530	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646883	125530	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88590646	125530	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646883	125530	0	None	-3019	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	938	17	13	10	-0.9	CCCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44413604	11817	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	551	8	2	5	3.6	CCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182065	11817	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	551	8	2	5	3.6	CCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL208953	11817	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	551	8	2	5	3.6	CCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		44409339	74996	0	None	630	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL203252	74996	0	None	630	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	723	19	6	5	3.7	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccccc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL3644302	211945	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	nan
		CHEMBL3644336	211976	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3644302	211945	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	nan
		CHEMBL3644336	211976	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL2415086	210437	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCC(=O)NC(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)(CCCNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		44447238	94920	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CS(=O)(=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254278	94920	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CS(=O)(=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		11398483	87248	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232973	87248	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44442942	93599	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL246605	93599	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	542	8	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4cccs4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11398483	87248	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232973	87248	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	532	13	0	5	7.1	COc1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44413741	12288	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	9	2	5	4.2	CC(=O)N1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184861	12288	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	9	2	5	4.2	CC(=O)N1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL373735	12288	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	9	2	5	4.2	CC(=O)N1CCC(CC(C)C)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44391285	64363	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	639	12	3	7	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL181277	64363	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	639	12	3	7	3.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCCn2ccnc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44455996	155460	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL403924	155460	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(Cl)c2)CC1	10.1016/j.bmcl.2007.10.115
		44347330	168063	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL432407	168063	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44455997	97838	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	11	1	6	4.4	COc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL272088	97838	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	11	1	6	4.4	COc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		44434880	88610	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235616	88610	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	477	10	2	2	6.4	NCC1CCCC(CN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		44434685	89171	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	497	14	3	3	6.3	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236638	89171	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	497	14	3	3	6.3	NCCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434691	89425	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	11	2	4	7.0	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL237069	89425	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	11	2	4	7.0	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434695	89426	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	503	9	2	2	7.1	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237070	89426	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	503	9	2	2	7.1	NC1CCC(CC2CCC(N(Cc3ccccc3F)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	89743	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434855	90030	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	90030	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44401371	71141	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	633	13	5	5	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL195548	71141	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	633	13	5	5	3.2	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562324	173406	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.1	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL452838	173406	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.1	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44395654	96573	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.7	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL263066	96573	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	12	2	6	3.7	CN(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44434579	89433	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	496	8	1	4	4.3	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237080	89433	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	496	8	1	4	4.3	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44447221	94669	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252584	94669	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	6	1	5	4.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416161	80408	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214551	80408	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		1338	3807	43	None	53	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44442934	93768	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247422	93768	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccco4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11156852	65685	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL183434	65685	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2008.07.076
		44562362	176839	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	505	9	2	4	5.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL461132	176839	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	505	9	2	4	5.3	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		88878679	147485	0	None	-25118	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1081	19	15	12	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3930415	147485	0	None	-25118	2	Human	6.4	pKi	=	6.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1081	19	15	12	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		11156852	65685	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL183434	65685	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44447237	94919	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254277	94919	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	606	9	1	6	3.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H]2CS(=O)(=O)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		70681742	75079	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035941	75079	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1ccc(Cl)cc1	10.1016/j.bmc.2012.04.001
		11156852	65685	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		CHEMBL183434	65685	0	None	-14	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	531	7	3	5	2.9	NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		44347082	163908	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL420727	163908	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	766	9	10	7	0.9	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44395465	66812	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	481	8	1	4	5.4	CC(C)(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		CHEMBL186030	66812	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	481	8	1	4	5.4	CC(C)(C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		44416093	80312	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	479	8	1	5	4.5	COc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL214155	80312	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	479	8	1	5	4.5	COc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		44434772	88597	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	88597	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434688	89173	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	13	2	2	5.4	NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236640	89173	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	405	13	2	2	5.4	NCCCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434855	90030	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238154	90030	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	7.5	CC1CC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		44434682	148604	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	451	13	2	2	6.1	NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393919	148604	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	451	13	2	2	6.1	NCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434847	88957	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	11	4	2	7.0	N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236442	88957	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	553	11	4	2	7.0	N=C(N)NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434545	148349	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL393715	148349	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44434545	148349	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL393715	148349	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	7	2	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](N)Cc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmc.2007.05.026
		24741964	89377	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236980	89377	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44562367	176928	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	563	8	2	5	5.8	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462010	176928	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	563	8	2	5	5.8	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)OC(C)(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44393417	96591	0	None	5	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL263182	96591	0	None	5	4	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	589	8	2	7	3.1	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2CCCCC2Cn2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		44433379	151701	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	622	6	1	5	6.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)OC(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL396429	151701	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	622	6	1	5	6.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)OC(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44416338	168880	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL438275	168880	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44442958	154781	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	8	1	6	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccn4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400162	154781	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	540	8	1	6	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4nccn4C)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44395416	122706	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL360422	122706	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	NC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL2415085	210436	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(=O)NCCCC(CCCNC(C)=O)(NC(=O)CNC(=O)Cn1cc(CCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(=O)NCCC(N)=O	10.1016/j.bmc.2013.06.052
		71450920	79038	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113143	79038	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		51346770	58227	0	None	-3	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
		CHEMBL1682209	58227	0	None	-3	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	643	11	2	8	3.5	COCC(=O)N[C@H]1Cc2ccc(OC)c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O	10.1016/j.bmcl.2011.01.011
		CHEMBL433645	213643	0	None	6	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		NC(=O)[C@H]1CCCCNC(=O)C[C@H](N)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N1	10.1021/jm010165y
		89007934	143054	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3895073	143054	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1067	18	17	12	-3.0	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644297	211940	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3646859	212003	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644328	211968	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	nan
		CHEMBL3644331	211971	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646875	212014	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646881	212020	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646889	212027	0	None	33	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		134142092	147193	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		CHEMBL3928099	147193	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1043	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](O)CN2C1=O	nan
		CHEMBL3644297	211940	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3644331	211971	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644344	211983	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646859	212003	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3646875	212014	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646881	212020	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646889	212027	0	None	33	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCNC(=O)CCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88287424	128650	0	None	575	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1058	18	17	12	-3.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667919	128650	0	None	575	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1058	18	17	12	-3.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663346	212076	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C(C)(C)C)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663355	212085	0	None	389	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3663362	212092	0	None	107	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663376	212105	0	None	6	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CN)NC1=O	nan
		CHEMBL3667920	212116	0	None	39	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667937	212131	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667946	212140	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3667948	212142	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667957	212151	0	None	20	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667960	212154	0	None	58	2	Human	8.4	pKi	=	8.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		122178168	121261	0	None	25	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577997	121261	0	None	25	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	963	12	10	10	-0.7	C[C@@H]1NC(=O)C(CCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577995	211752	0	None	6	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3578000	211754	0	None	50	2	Mouse	8.4	pKi	=	8.4	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		25132866	172611	0	None	77	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
		CHEMBL449131	172611	0	None	77	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1ccncc1	10.1021/jm800525p
		44569175	188822	0	None	32	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
		CHEMBL506272	188822	0	None	32	3	Human	8.4	pKi	=	8.4	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	2.5	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCC(=O)N1	10.1021/jm800525p
		44412560	139470	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	593	11	2	5	4.1	CCN(CC)CC(C1CCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379423	139470	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	593	11	2	5	4.1	CCN(CC)CC(C1CCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		44412561	139725	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	11	2	5	4.5	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL379823	139725	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	11	2	5	4.5	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2006.04.002
		11993702	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		5416	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		9272	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		CHEMBL3301624	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		DB11700	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.1c00095
		44577062	193374	0	None	26	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL525177	193374	0	None	26	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	4.6	CNCC(=O)N[C@H](c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		44432952	87044	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232584	87044	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44562477	186730	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	9	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488710	186730	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	533	9	3	5	3.8	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		6918850	125422	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL364560	125422	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2006.04.069
		44432952	87044	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232584	87044	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	518	13	1	6	6.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3cccnc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		6918850	125422	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL364560	125422	1	None	154	4	Human	8.4	pKi	=	8.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1ccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		42630327	155871	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
		CHEMBL4060381	155871	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1119	32	19	14	-3.3	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CS)C(N)=O	10.1021/acs.jmedchem.8b00170
		11993702	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		5416	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		9272	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		CHEMBL3301624	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		DB11700	3593	18	None	-1	5	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		None	10.1021/acs.jmedchem.2c00793
		CHEMBL407213	212648	0	None	44	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL		None	None	None		CC(=O)N[C@H]1CC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC1=O	10.1021/jm010165y
		10324857	75992	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL205468	75992	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	534	12	2	4	4.9	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL2331674	209532	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)CCc1cn(CC(=O)NCCCC(CCCNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)(NC(=O)CNC(=O)Cn2cc(CCC(=O)N[C@@H](Cc3cnc[nH]3)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(N)=O)nn2)C(=O)NCCC(N)=O)nn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/j.bmc.2013.06.052
		56851059	69074	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		57390568	69074	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		91930628	69074	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		CHEMBL1923668	69074	0	None	-1	3	Human	8.4	pKi	=	8.4	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	1784	57	24	20	-1.4	C#CCCCC(=O)NCCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](CCCC)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)C(C)C	10.1021/jm201226w
		44444499	155013	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL401466	155013	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	571	8	2	5	4.4	CC(C)[C@H](NC(=O)[C@@H](C)N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44432924	87278	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233156	87278	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		44433264	89351	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236940	89351	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400863	69164	0	None	151	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	602	11	2	6	5.8	CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL192464	69164	0	None	151	3	Human	8.4	pKi	=	8.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	602	11	2	6	5.8	CC(C)OC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		166585313	192175	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		CHEMBL5204022	192175	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	4	1	9	2.8	COc1cc([C@@H](C)C(=O)N2CC[C@]3(CCc4cc(-c5nnn(C)n5)c(C)nc4N3)C2)c(Cl)cn1	10.1021/acsmedchemlett.2c00229
		44434568	89176	0	None	81	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236650	89176	0	None	81	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	613	8	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCNCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44433264	89351	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236940	89351	0	None	56	3	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	598	8	1	4	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44433563	88716	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	584	7	1	4	5.6	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236064	88716	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	584	7	1	4	5.6	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.09.079
		44432924	87278	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233156	87278	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	559	14	1	6	7.4	CC(=O)c1cccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)c1	10.1016/j.bmcl.2007.06.010
		CHEMBL2370967	209970	0	None	2	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44400932	70303	0	None	173	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	588	11	2	6	5.4	CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL194393	70303	0	None	173	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	588	11	2	6	5.4	CCOC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL2070242	209183	0	None	1	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)CNC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44456304	155254	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		CHEMBL402787	155254	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	10	1	5	4.7	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		1338	3807	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44562495	186634	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	561	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488030	186634	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	561	10	3	5	4.4	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44444495	154915	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL400932	154915	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44456219	155438	0	None	25	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL403806	155438	0	None	25	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	637	10	1	6	5.0	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44444495	154915	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL400932	154915	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		11215758	66079	0	None	125	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL183799	66079	0	None	125	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	624	9	3	6	5.0	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cnc3ccccc3c2)CC1	10.1016/j.bmcl.2004.10.096
		44432909	168969	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL439020	168969	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44444507	94173	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL249571	94173	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44432909	168969	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL439020	168969	1	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	545	14	1	6	7.0	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44433283	96460	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL262320	96460	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	684	13	2	5	6.4	CC(C)C[C@H](NCCCC(=O)O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44395667	66965	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	12	3	6	4.3	O=C(CC1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186737	66965	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	12	3	6	4.3	O=C(CC1CCCN1)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644333	211973	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		134148066	149973	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1068	18	17	12	2.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](Cc2cnc[nH]2)/N=C\1O	nan
		CHEMBL3949976	149973	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1068	18	17	12	2.7	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](Cc2cnc[nH]2)/N=C\1O	nan
		CHEMBL3667932	212126	0	None	100	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44447240	94950	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254490	94950	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.3	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL267492	210724	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]2CCCN2C1=O	10.1021/jm050780s
		44447806	95550	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	532	6	1	5	3.8	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3S(C)(=O)=O)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL257579	95550	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	532	6	1	5	3.8	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3S(C)(=O)=O)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44404564	126441	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccccc1C(F)(F)F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL365184	126441	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	343	6	0	3	3.3	CCN(CC)CC(c1ccccc1C(F)(F)F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404561	134858	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	7	0	3	2.2	CCN(CC)CC(Cc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL371896	134858	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	7	0	3	2.2	CCN(CC)CC(Cc1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		6918857	138709	1	None	33	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL377961	138709	1	None	33	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	11	2	5	4.4	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2005.10.103
		44415388	80586	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	12	2	5	5.2	NCCNC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL214988	80586	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	12	2	5	5.2	NCCNC(COCc1ccccc1)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		70688111	75081	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	494	9	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035943	75081	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	494	9	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		44397133	66717	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	671	11	3	6	4.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL185625	66717	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	671	11	3	6	4.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)c3ccc(OC(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415347	141903	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		CHEMBL386868	141903	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	477	8	1	4	5.0	COc1cccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c1	10.1016/j.bmcl.2006.05.088
		44416024	80112	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	477	7	1	4	5.1	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL213214	80112	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	477	7	1	4	5.1	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		44434843	88700	0	None	1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236020	88700	0	None	1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	587	11	4	2	7.6	N=C(N)NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	89743	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		51346771	58226	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
		CHEMBL1682208	58226	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor expressed in BHK cells	ChEMBL	671	10	2	9	3.3	COCC(=O)N[C@H]1Cc2cc3c(c(c2)Cc2ccc(cc2)Oc2cccc(c2)CN(CCCN2CCN(CCCN)CC2)C1=O)OCOC3	10.1016/j.bmcl.2011.01.011
		CHEMBL438596	213781	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44391315	63907	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	659	14	3	6	5.1	CC(C)COCCCNC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL180545	63907	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	659	14	3	6	5.1	CC(C)COCCCNC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44396002	124774	0	None	17	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	587	11	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1	10.1016/j.bmcl.2004.08.055
		CHEMBL364215	124774	0	None	17	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	587	11	2	6	4.8	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1cccnc1	10.1016/j.bmcl.2004.08.055
		168279695	191135	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5188196	191135	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44413606	11820	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(C)C1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182088	11820	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(C)C1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211032	11820	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(C)C1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		44395535	126386	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	628	12	2	6	4.5	O=C([C@@H](Cc1ccc(Cl)cc1)NS(=O)(=O)CC(F)(F)F)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL365082	126386	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	628	12	2	6	4.5	O=C([C@@H](Cc1ccc(Cl)cc1)NS(=O)(=O)CC(F)(F)F)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44447243	154791	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL400191	154791	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		71452734	79041	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	7	3	5	3.4	CC(=O)NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113146	79041	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	613	7	3	5	3.4	CC(=O)NC1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		10077483	77323	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	610	13	2	4	7.1	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)Nc1ccccc1	10.1016/j.bmcl.2006.01.016
		CHEMBL208329	77323	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	610	13	2	4	7.1	CCN(CC)CCCC(C)/N=C(\NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC)Nc1ccccc1	10.1016/j.bmcl.2006.01.016
		44415940	80952	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	467	8	1	3	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215354	80952	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	467	8	1	3	6.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		44434704	89172	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236639	89172	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	605	11	3	3	8.6	Cc1ccccc1CN(C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434690	89306	0	None	-4	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	89306	0	None	-4	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434713	89596	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237502	89596	0	None	-2	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		11845438	137623	0	None	3	3	Human	6.4	pKi	=	6.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL375775	137623	0	None	3	3	Human	6.4	pKi	=	6.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	661	12	6	6	2.4	N=C(N)NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm060384p
		25217223	166590	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL428014	166590	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		44562366	176927	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	3	4	4.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)NC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462009	176927	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	546	9	3	4	4.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)NC2CC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3646887	212025	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646887	212025	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44405366	71961	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		CHEMBL197327	71961	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	643	12	3	5	4.7	NC(CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		44447823	155043	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401631	155043	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	6	1	5	5.0	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44347378	114435	0	None	5	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	818	11	11	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL333262	114435	0	None	5	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	818	11	11	9	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44400769	127512	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	632	12	2	6	6.4	O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL366171	127512	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	632	12	2	6	6.4	O=C(N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44412909	78232	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1C	10.1016/j.bmcl.2006.04.069
		CHEMBL210600	78232	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1C	10.1016/j.bmcl.2006.04.069
		44444437	94408	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL250991	94408	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3ccnn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		25217223	166590	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		CHEMBL428014	166590	1	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	15	2	8	5.7	COc1cc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc(OC)c1OC	10.1016/j.bmcl.2007.06.010
		44397223	67117	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	636	10	4	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL187439	67117	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	636	10	4	5	4.7	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc(Cl)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415941	140161	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL380299	140161	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	517	7	1	4	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		24882666	95718	0	None	-1	2	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	385	10	5	3	1.7	N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		CHEMBL258295	95718	0	None	-1	2	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	385	10	5	3	1.7	N=C(N)NCCC[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		71461657	79039	0	None	-15	4	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	556	6	2	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113144	79039	0	None	-15	4	Human	5.4	pKi	=	5.4	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	556	6	2	4	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3c2CCCC3)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		9946241	89432	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.1	NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL237079	89432	0	None	-10	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.1	NCCN(C(=O)Cc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL3644282	211926	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644282	211926	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3644289	211933	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O	nan
		CHEMBL3644330	211970	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644289	211933	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O	nan
		CHEMBL3644330	211970	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44433475	148889	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL394160	148889	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	514	7	1	4	5.2	CC(C)CN1C[C@@H](C(=O)N2CCN(c3c(F)cccc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44447249	155517	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL404207	155517	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	554	9	1	5	4.6	Cc1ccc(N2CCN(C(=O)[C@H]3OCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		168285313	191401	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5192562	191401	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168283616	191239	0	None	-20	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5190042	191239	0	None	-20	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2110	33	32	25	-4.5	CCCC[C@@H]1NC(=O)[C@@H]2CSCC(=O)CSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44413652	12300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	613	9	2	5	4.5	CN1CCC(Cc2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184921	12300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	613	9	2	5	4.5	CN1CCC(Cc2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL378415	12300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	613	9	2	5	4.5	CN1CCC(Cc2ccccc2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		44396069	66261	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	602	10	2	6	3.9	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(c2ccccc2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184643	66261	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	602	10	2	6	3.9	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(c2ccccc2)CC1	10.1016/j.bmcl.2004.08.055
		44443005	94522	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL251698	94522	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	565	8	2	5	3.9	CC(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44415790	80090	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1OC	10.1016/j.bmcl.2006.05.088
		CHEMBL213125	80090	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	507	9	1	5	5.1	COc1ccc(CCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1OC	10.1016/j.bmcl.2006.05.088
		44434699	89500	0	None	-1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	531	10	2	3	7.7	CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237290	89500	0	None	-1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	531	10	2	3	7.7	CSc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		44413968	80229	0	None	-229	3	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL213751	80229	0	None	-229	3	Human	5.4	pKi	=	5.4	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		11296732	143813	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL390130	143813	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44435184	148191	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	476	7	1	4	5.3	Cc1ccc([C@H](N)CC(C)C)c(N2CCN(C(=O)C(C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		CHEMBL393583	148191	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	476	7	1	4	5.3	Cc1ccc([C@H](N)CC(C)C)c(N2CCN(C(=O)C(C)Cc3ccc(Cl)cc3Cl)CC2)n1	10.1021/jm701137s
		11296732	143813	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL390130	143813	0	None	22	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	539	11	3	6	3.1	NCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44443021	94121	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL249267	94121	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	554	8	1	4	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(F)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		168295173	192311	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5206293	192311	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168270124	189955	0	None	-33	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5170533	189955	0	None	-33	3	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2096	33	32	24	-3.6	CCCC[C@@H]1NC(=O)[C@@H]2CSCCCSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44432960	87300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233175	87300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44322924	107112	0	None	-3	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL316038	107112	0	None	-3	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	701	19	11	8	-1.4	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CO)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44412685	79740	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)OCc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL211680	79740	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)OCc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		44416092	79806	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	463	7	1	4	4.8	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		CHEMBL212024	79806	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	463	7	1	4	4.8	Cc1ccc(OCC(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2006.06.075
		44434778	89743	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434709	89775	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	563	9	2	2	7.7	NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237714	89775	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	563	9	2	2	7.7	NC1CCC(CC2CCC(N(Cc3ccccc3Br)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434863	148144	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393552	148144	0	None	-1	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	9	2	2	5.3	NCC1CCC(CN(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44434665	147949	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393383	147949	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265347	96967	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	10	4	4	3.3	NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL266305	96967	0	None	-1	4	Human	4.4	pKi	=	4.4	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	10	4	4	3.3	NCCNC(=O)[C@H](CNCc1ccc2ccccc2c1)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		44413592	78417	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL211131	78417	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	767	10	10	7	1.6	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL3644320	211960	0	None	75	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646874	212013	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644320	211960	0	None	75	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646874	212013	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663328	212060	0	None	-1	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C#N)NC(=O)[C@H](CCN)NC1=O	nan
		52919529	152619	0	None	-4466	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1038	19	14	11	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3972160	152619	0	None	-4466	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1038	19	14	11	-0.6	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88944180	152678	0	None	-2951	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	987	20	14	11	-1.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3972716	152678	0	None	-2951	2	Human	7.4	pKi	=	7.4	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	987	20	14	11	-1.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		168279695	191135	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5188196	191135	0	None	-1	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	66	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44432960	87300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233175	87300	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	13	0	6	6.9	COC(=O)c1ccc(-c2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		25217225	152289	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL396940	152289	1	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		44447807	168734	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	6	1	5	3.7	COc1ccc([C@H]2CCN(C(C)=O)[C@H]2C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)cc1	10.1016/j.bmcl.2008.01.125
		CHEMBL437032	168734	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	6	1	5	3.7	COc1ccc([C@H]2CCN(C(C)=O)[C@H]2C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)cc1	10.1016/j.bmcl.2008.01.125
		44397124	123683	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	641	11	3	5	5.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL362158	123683	0	None	-	1	Human	7.4	pKi	=	7.4	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	641	11	3	5	5.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(C(F)(F)F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168272660	190433	0	None	-57	3	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5178164	190433	0	None	-57	3	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2202	33	32	24	-2.1	CCCC[C@@H]1NC(=O)[C@@H]2CSc3c(F)c(F)c(c(F)c3F)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		25217225	152289	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL396940	152289	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	574	14	1	7	6.2	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		44412678	138669	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377762	138669	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	614	11	3	6	3.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Cc2ccccc2F)CC1	10.1016/j.bmcl.2006.04.069
		44444468	154658	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	567	10	1	5	4.4	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(=O)CCN	10.1016/j.bmcl.2007.06.088
		CHEMBL399557	154658	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	567	10	1	5	4.4	CC(C)CN(Cc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(=O)CCN	10.1016/j.bmcl.2007.06.088
		44416023	80111	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL213213	80111	0	None	-	1	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	483	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccccc2Cl)CC1	10.1016/j.bmcl.2006.06.075
		44434700	149509	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	637	12	3	4	9.0	CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL394645	149509	0	None	1	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	637	12	3	4	9.0	CSc1ccc(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1	10.1016/j.bmc.2007.06.003
		88878636	152851	0	None	-114	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	944	17	13	10	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3974162	152851	0	None	-114	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	944	17	13	10	-1.4	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		168285904	191670	0	None	-9	3	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5196407	191670	0	None	-9	3	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2cccc(c2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44562458	179019	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.2	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471166	179019	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	9	3	5	4.2	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44395466	66961	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.6	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3CNCCc3cccs3)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186732	66961	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.6	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(c3ccccc3CNCCc3cccs3)CC2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644319	211959	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		CHEMBL3644319	211959	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O	nan
		44413932	137546	0	None	1	3	Human	7.3	pKi	=	7.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
		CHEMBL375440	137546	0	None	1	3	Human	7.3	pKi	=	7.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	570	12	5	5	3.1	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1	10.1021/jm060384p
		44413687	12291	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	564	9	2	4	5.5	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1184874	12291	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	564	9	2	4	5.5	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL375389	12291	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	564	9	2	4	5.5	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL443590	213925	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CC(C)[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CNC1=O	10.1021/jm030119t
		11353522	57182	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL164884	57182	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	560	8	2	5	4.2	CC(C)Oc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44415725	77949	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	453	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccs2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209601	77949	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	453	7	1	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2cccs2)CC1	10.1016/j.bmcl.2006.05.088
		44416108	80836	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	465	7	2	5	4.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(O)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215238	80836	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	465	7	2	5	4.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)COc2ccc(O)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44443012	94004	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	8	2	5	4.1	CCNC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248670	94004	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	8	2	5	4.1	CCNC(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44404540	72393	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	279	4	1	3	1.3	CC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198665	72393	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	279	4	1	3	1.3	CC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44562519	194545	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CCC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL529449	194545	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CCC(C)C(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44391379	63481	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.9	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL179889	63481	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.9	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2(N)CCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644313	211953	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@](C)(Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644313	211953	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@](C)(Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44434552	89293	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c([C@H](N)CC(C)C)cccc2C(F)(F)F)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236838	89293	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	572	8	2	4	5.5	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c([C@H](N)CC(C)C)cccc2C(F)(F)F)CC1	10.1016/j.bmc.2007.05.026
		44444490	94506	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	7	1	4	5.3	CC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		CHEMBL251587	94506	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	538	7	1	4	5.3	CC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmcl.2007.06.088
		44444508	155082	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL401853	155082	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	9	2	5	5.7	CC(C)C[C@H](NC(=O)[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44415965	79912	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212451	79912	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44401553	69825	0	None	18	2	Human	7.3	pKi	=	7.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	648	14	4	5	3.7	COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1	10.1016/j.bmcl.2005.03.120
		CHEMBL193715	69825	0	None	18	2	Human	7.3	pKi	=	7.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	648	14	4	5	3.7	COc1ccc(CNC(=O)[C@@H]2C[C@@H](Cc3ccccc3)CN2C(=O)[C@H](CCCN=C(N)N)NC(=O)Cc2cccc3ccccc23)cc1	10.1016/j.bmcl.2005.03.120
		44396067	66232	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	548	10	4	6	3.8	CC(Nc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL184542	66232	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	548	10	4	6	3.8	CC(Nc1ccccc1N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1	10.1016/j.bmcl.2004.08.055
		44455956	155036	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	10	1	5	4.7	Cc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL401593	155036	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	10	1	5	4.7	Cc1cccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3c(F)cccc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)c1	10.1016/j.bmcl.2007.10.115
		88944290	149199	0	None	-4677	2	Human	5.3	pKi	=	5.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3943941	149199	0	None	-4677	2	Human	5.3	pKi	=	5.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	996	19	14	11	-1.2	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44434778	89743	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434655	90022	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	12	2	2	5.6	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238135	90022	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	417	12	2	2	5.6	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44404538	72363	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	315	5	1	4	0.7	CN1CCN(C(CNS(C)(=O)=O)c2ccccc2F)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198544	72363	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	315	5	1	4	0.7	CN1CCN(C(CNS(C)(=O)=O)c2ccccc2F)CC1	10.1016/j.bmcl.2005.08.018
		46905545	10300	0	None	2	2	Human	5.3	pKi	=	5.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	631	14	7	6	1.4	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL1161792	10300	0	None	2	2	Human	5.3	pKi	=	5.3	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	631	14	7	6	1.4	CC(N)=O.N=C(N)NCCC[C@H](NC(=O)CCc1c[nH]cn1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		137658158	159717	0	None	-16	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4104465	159717	0	None	-16	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1714	21	22	21	-3.6	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44395899	169320	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL441675	169320	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	565	11	3	6	3.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3663344	212074	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(N)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3667935	212129	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		168285313	191401	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5192562	191401	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		46885711	8070	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
		CHEMBL1091150	8070	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	504	3	1	3	5.4	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccc(Cl)cc1	10.1021/jm9017866
		44447248	94702	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL252825	94702	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	9	1	5	4.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412910	138373	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(C)(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377186	138373	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	11	4	7	2.0	CC(C)(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL2370966	209969	0	None	-39	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](CCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44444427	154409	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	436	4	0	4	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C#N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL398854	154409	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	436	4	0	4	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3C#N)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44416074	139538	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	468	8	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCNC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL379591	139538	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	468	8	2	4	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCNC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		44435220	89252	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	10	2	3	8.9	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236803	89252	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	609	10	2	3	8.9	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)c3cc4cc(OCc5ccccc5)ccc4[nH]3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434715	167508	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	593	10	2	3	7.8	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		CHEMBL429983	167508	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	593	10	2	3	7.8	COc1ccc(CN(C(=O)CCCc2c[nH]c3ccccc23)C2CCC(CC3CCC(N)CC3)CC2)cc1Br	10.1016/j.bmc.2007.06.003
		71458056	79030	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	541	6	3	4	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3cc[nH]c23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113135	79030	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	541	6	3	4	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2cccc3cc[nH]c23)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2005.07.035
		44404577	71953	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	295	4	1	4	1.5	COC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL197289	71953	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	295	4	1	4	1.5	COC(=O)NCC(c1ccccc1F)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		2683	102888	25	None	-676	16	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL305906	102888	25	None	-676	16	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		CHEMBL334255	102888	25	None	-676	16	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	304	15	0	0	6.5	CCCCCCCCCCCCCCCC[n+]1ccccc1	nan
		44433273	89670	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	4.9	CNCCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237577	89670	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	605	12	2	5	4.9	CNCCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44562598	174261	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	9	3	5	4.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCCNC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454917	174261	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	574	9	3	5	4.4	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C2CCCNC2)CC1	10.1016/j.bmcl.2008.07.076
		44323031	168078	0	None	-8	3	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL432565	168078	0	None	-8	3	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	775	21	10	7	1.2	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391402	123652	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2cccnc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL361985	123652	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2cccnc2)CC1	10.1016/j.bmcl.2004.10.096
		168295173	192311	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5206293	192311	0	None	-1	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2967	62	33	39	-5.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CC(C)C)CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC2=O)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44393851	123089	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL360989	123089	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	2	6	3.5	COCCN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44434554	89403	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237049	89403	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	587	9	3	5	4.4	CC(C)C[C@@H](N)c1cccc(C(F)(F)F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		71452721	78973	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	580	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3nccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL2113035	78973	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	580	11	3	7	3.5	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3nccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415521	141435	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL384138	141435	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		44393876	122567	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL360169	122567	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	603	11	4	6	3.0	O=C(O)CCNCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44415521	141435	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384138	141435	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	473	5	1	3	5.3	CC(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44444438	154855	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cccn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400595	154855	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	491	6	0	5	4.4	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cccn3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44397054	125791	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	9	3	5	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C(F)(F)F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL364772	125791	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	579	9	3	5	2.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)C(F)(F)F)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44415746	79837	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(S(C)(=O)=O)cc2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212146	79837	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	525	8	1	5	4.4	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(S(C)(=O)=O)cc2)CC1	10.1016/j.bmcl.2006.05.088
		44434713	89596	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237502	89596	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	541	11	2	3	7.5	COc1ccccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434584	151942	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	394	6	1	3	4.9	NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL396638	151942	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	394	6	1	3	4.9	NCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CCCCC2)CC1	10.1016/j.bmc.2007.06.003
		11845630	139514	0	None	5	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL379490	139514	0	None	5	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	678	15	5	6	3.6	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		44433295	89084	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236520	89084	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.6	CC(C)C[C@H](NC(=O)CCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44400812	71300	0	None	457	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	667	12	3	5	6.3	O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL195734	71300	0	None	457	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	667	12	3	5	6.3	O=C(NCc1ccccc1F)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44400778	135888	0	None	162	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	574	10	2	6	5.0	COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL373099	135888	0	None	162	2	Human	8.3	pKi	=	8.3	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	574	10	2	6	5.0	COC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44409338	168744	0	None	1230	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		CHEMBL437132	168744	0	None	1230	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	739	19	7	6	3.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC[C@H](Cc1ccc(O)cc1)NC(C)=O)Cc1ccc(F)cc1	10.1016/j.bmcl.2005.12.005
		44415918	141549	0	None	-2	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL384774	141549	0	None	-2	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	754	16	6	7	0.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(C)=O)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44323029	207181	0	None	-1	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL92481	207181	0	None	-1	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	795	20	10	7	1.5	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL3644279	211923	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644329	211969	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](N)CN2C1=O	nan
		CHEMBL3646880	212019	0	None	25	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646885	212023	0	None	47	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646892	212030	0	None	51	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		134134506	143676	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3900116	143676	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3644279	211923	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646880	212019	0	None	25	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646885	212023	0	None	47	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646892	212030	0	None	51	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663359	212089	0	None	173	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663380	212109	0	None	8	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3663382	212111	0	None	25	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667921	212117	0	None	81	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667934	212128	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667936	212130	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667955	212149	0	None	20	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667962	212156	0	None	107	2	Human	8.3	pKi	=	8.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		122178169	121262	0	None	31	2	Mouse	8.3	pKi	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577998	121262	0	None	31	2	Mouse	8.3	pKi	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	977	13	10	10	-0.4	C[C@@H]1NC(=O)C(CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577999	211753	0	None	19	2	Mouse	8.3	pKi	=	8.3	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44413668	139516	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	621	13	2	5	5.4	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL379497	139516	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	621	13	2	5	5.4	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2006.04.016
		1338	3807	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44432930	167481	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL429943	167481	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44569176	172545	0	None	19	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
		CHEMBL448410	172545	0	None	19	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.3	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H]1CCCCN1	10.1021/jm800525p
		25133209	173351	0	None	53	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
		CHEMBL452710	173351	0	None	53	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	589	12	3	5	2.4	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)CNC	10.1021/jm800525p
		44412574	78055	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209990	78055	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCN(CC)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44412642	138682	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	13	2	5	5.6	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL377825	138682	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	13	2	5	5.6	CCN(CC)CC(CC1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44432930	167481	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL429943	167481	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.2	COc1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		44410188	140380	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
		CHEMBL380854	140380	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	568	12	2	3	5.3	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1ccccc1	10.1016/j.bmcl.2006.01.016
		44432948	150231	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395227	150231	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		25133556	188849	0	None	3	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
		CHEMBL506762	188849	0	None	3	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C1CCNCC1	10.1021/jm800525p
		44432948	150231	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL395227	150231	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	593	14	1	5	8.9	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(-c4ccccc4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL428326	213438	0	None	-10	4	Human	8.3	pKi	=	8.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)CN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm0501432
		44416152	81098	0	None	38	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL215576	81098	0	None	38	3	Human	8.3	pKi	=	8.3	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	560	11	3	4	2.4	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)CCc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		44456027	155470	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL403967	155470	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	599	10	1	5	5.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.10.115
		44456259	167266	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	566	7	0	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL429314	167266	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	566	7	0	5	5.5	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@H](C(C)C)N(C)C)c1	10.1016/j.bmcl.2007.10.115
		44577059	193327	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	536	9	2	4	4.7	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL524443	193327	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	536	9	2	4	4.7	CNCC(=O)N[C@H](c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2Cl)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		10304794	139405	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL379352	139405	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	635	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44433446	151964	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL396660	151964	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	593	8	1	5	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCN(CC(C)C)CC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44577063	188100	0	None	70	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL498150	188100	0	None	70	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	544	8	1	4	4.9	CC(C)[C@H](NC(=O)C1CN(C)C1)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44577060	188052	0	None	-1	8	Rat	8.3	pKi	=	8.3	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL497746	188052	0	None	-1	8	Rat	8.3	pKi	=	8.3	Binding	Binding affinity at rat MC4RBinding affinity at rat MC4R	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		23661656	169044	0	None	1	5	Mouse	8.3	pKi	=	8.3	Binding	Binding affinity to C57BL/6J mouse MC4 receptorBinding affinity to C57BL/6J mouse MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL439560	169044	0	None	1	5	Mouse	8.3	pKi	=	8.3	Binding	Binding affinity to C57BL/6J mouse MC4 receptorBinding affinity to C57BL/6J mouse MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44442997	93922	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		CHEMBL248205	93922	0	None	-	1	Human	8.3	pKi	=	8.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	576	8	1	4	6.3	O=C([C@H]1CN(C2CCCCC2)C[C@@H]1c1ccc(Cl)cc1)N1CCN(C2(CNCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2007.10.032
		25129453	171766	0	None	14	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
		CHEMBL446757	171766	0	None	14	3	Human	8.3	pKi	=	8.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	677	11	3	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@@H]1Cc2ccccc2CN1	10.1021/jm800525p
		CHEMBL2370964	209967	0	None	-7	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44322795	206926	0	None	13	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL91041	206926	0	None	13	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	853	11	12	9	-0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		16007263	79796	0	None	41	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL211975	79796	0	None	41	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	557	11	4	5	1.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccccc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		23635236	91601	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		23635236	91601	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
		CHEMBL240780	91601	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL240780	91601	0	None	60	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	512	10	2	4	4.6	CNCCC(=O)N[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1)C(C)C	10.1021/jm070806a
		44432956	148583	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL393903	148583	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		10283036	140243	0	None	72	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	647	11	2	5	5.2	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380540	140243	0	None	72	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	647	11	2	5	5.2	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C2Cc3ccccc3C(C)(C)N2)CC1	10.1016/j.bmcl.2005.10.103
		44432956	148583	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL393903	148583	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	573	15	1	6	7.3	CC(=O)c1ccc(CNc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN2CCCCC2)cc1	10.1016/j.bmcl.2007.06.010
		23635237	91453	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635237	91453	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
		CHEMBL240364	91453	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL240364	91453	0	None	45	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	498	9	2	4	4.3	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN)C(C)C)c1	10.1021/jm070806a
		44416286	138912	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	455	7	1	3	5.5	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL378327	138912	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	455	7	1	3	5.5	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		44395869	67236	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	579	11	3	6	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL187957	67236	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	579	11	3	6	3.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3646888	212026	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3646888	212026	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44432917	172722	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL450577	172722	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		46885481	7755	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089104	7755	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnc3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44404547	135794	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL373042	135794	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)C[C@@H](c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		71454510	79049	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113154	79049	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		168287698	191797	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5198280	191797	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5077144	214485	0	None	-32	3	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44432917	172722	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL450577	172722	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	531	11	1	6	6.8	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2C2CCN(C)CC2)cc1	10.1016/j.bmcl.2007.06.010
		44562440	179041	0	None	27	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471340	179041	0	None	27	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		71450919	79031	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.3	CC(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113136	79031	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.3	CC(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44434663	88515	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	483	13	3	3	5.9	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235138	88515	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	483	13	3	3	5.9	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434778	89743	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		10109225	154672	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	3	3.2	NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL399624	154672	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	3	3.2	NCCCN(C/C=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		70690145	75069	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	420	8	3	4	1.6	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CNC[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035931	75069	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	420	8	3	4	1.6	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CNC[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		44265496	97049	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		CHEMBL267020	97049	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki valueBinding affinity towards Melanocortin 4 receptor, expressed as negative log of the Ki value	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1021/jm020945m
		CHEMBL3644288	211932	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644288	211932	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O	nan
		44455893	155638	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL404706	155638	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)c(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44432902	147627	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL393134	147627	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		44432902	147627	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL393134	147627	1	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	505	14	2	6	6.1	CNCCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		88944368	143502	0	None	-2630	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3898758	143502	0	None	-2630	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44444449	154089	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	1	4	4.9	CC(C)CNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL398488	154089	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	496	8	1	4	4.9	CC(C)CNCc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44442900	93738	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247229	93738	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	564	8	1	4	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44391386	131448	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	616	11	4	6	3.7	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL369104	131448	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	616	11	4	6	3.7	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccc2)CC1	10.1016/j.bmcl.2004.10.096
		11157584	168244	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL433710	168244	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	587	10	2	5	4.3	CCN(CC)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44447820	95511	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.1	CCCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257374	95511	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.1	CCCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44447773	95706	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL258245	95706	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3NCC[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44443025	94123	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	6	5.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc([N+](=O)[O-])cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL249269	94123	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	6	5.3	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc([N+](=O)[O-])cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		46885523	7803	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		CHEMBL1089461	7803	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	493	4	1	6	3.4	C[C@H]1CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccn1	10.1021/jm9017866
		44412964	77368	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	522	11	4	7	1.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCO)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208553	77368	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	522	11	4	7	1.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNCCO)CC1	10.1016/j.bmcl.2006.04.069
		44444425	94140	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	5	0	4	4.1	COc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL249348	94140	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	5	0	4	4.1	COc1ccccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44444454	94146	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNC3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL249376	94146	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	495	7	2	5	3.2	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CNC3CNC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44396956	124379	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	643	10	3	5	4.9	CC(C)(C)c1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL363877	124379	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	643	10	3	5	4.9	CC(C)(C)c1ccc(C(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44434690	89306	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	89306	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44562391	189845	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	504	9	2	4	5.3	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL516659	189845	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	504	9	2	4	5.3	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		71456243	78962	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	8	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113020	78962	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	601	8	2	6	3.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCOCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		44394078	161717	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL413556	161717	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	611	10	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCc2ccco2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44447781	155264	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL402822	155264	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		168293467	192151	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5203840	192151	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		11262020	120267	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL352457	120267	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	612	9	2	7	3.7	Cn1ccnc1COc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		71459941	79042	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.2	CN(C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1)S(C)(=O)=O	10.1016/j.bmcl.2005.07.035
		CHEMBL2113147	79042	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.2	CN(C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1)S(C)(=O)=O	10.1016/j.bmcl.2005.07.035
		44434867	88523	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235162	88523	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		44434769	89739	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	659	11	3	3	9.6	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237698	89739	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	659	11	3	3	9.6	NC1CCC(CC2CCC(N(Cc3c(Cl)cccc3Cl)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		70694364	75075	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	304	5	4	5	-1.1	NCCNC(=O)[C@@H]1CNC[C@H]1C(=O)NC(=O)c1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035937	75075	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	304	5	4	5	-1.1	NCCNC(=O)[C@@H]1CNC[C@H]1C(=O)NC(=O)c1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL3644284	211928	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644284	211928	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88944367	148290	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3936714	148290	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1044	18	14	11	-1.4	CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44562520	191739	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	568	10	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)Cc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL519729	191739	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	568	10	3	5	4.0	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)Cc2ccccc2)CC1	10.1016/j.bmcl.2008.07.076
		137637711	155846	0	None	-20	3	Mouse	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting methodDisplacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting method	ChEMBL	871	11	14	12	-3.9	C[C@@H]1NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC1=O	10.1021/acs.jmedchem.7b00856
		CHEMBL4060087	155846	0	None	-20	3	Mouse	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting methodDisplacement of [125I]-NDP-R-MSH from mouse melanocortin receptor 4 expressed in HEK293 cells after 2 hrs by scintillation counting method	ChEMBL	871	11	14	12	-3.9	C[C@@H]1NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CS)NC1=O	10.1021/acs.jmedchem.7b00856
		168287698	191797	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5198280	191797	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44447810	155033	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	5	1	4	4.7	CC(=O)N1CC[C@H](c2ccc(C(F)(F)F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL401584	155033	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	5	1	4	4.7	CC(=O)N1CC[C@H](c2ccc(C(F)(F)F)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44412665	77870	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	578	10	2	4	5.9	CC(C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		CHEMBL209325	77870	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	578	10	2	4	5.9	CC(C)CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1	10.1016/j.bmcl.2006.04.002
		44443035	154417	0	None	-26	4	Human	6.3	pKi	=	6.3	Binding	Binding affinity to MC5RBinding affinity to MC5R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		CHEMBL398929	154417	0	None	-26	4	Human	6.3	pKi	=	6.3	Binding	Binding affinity to MC5RBinding affinity to MC5R	ChEMBL	584	9	1	5	5.5	COc1ccc(CNCC2(N3CCN(C(=O)[C@H]4CN(C(C)C)C[C@@H]4c4ccc(Cl)cc4)CC3)CCCCC2)cc1F	10.1016/j.bmcl.2007.10.032
		53236832	151913	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1002	19	13	12	-0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3966176	151913	0	None	-1548	2	Human	6.3	pKi	=	6.3	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1002	19	13	12	-0.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44433420	88670	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	542	5	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235893	88670	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	542	5	1	4	5.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(=O)C(C)(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44397226	161663	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	647	11	4	7	3.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL413064	161663	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	647	11	4	7	3.9	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44395534	66761	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.5	NC(CC(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		CHEMBL185852	66761	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.5	NC(CC(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)c1ccc(Cl)cc1	10.1016/j.bmcl.2004.08.055
		44434633	89170	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	423	11	2	2	5.3	NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236630	89170	0	None	-2	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	423	11	2	2	5.3	NCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265496	97049	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL267020	97049	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	453	9	3	3	3.9	NC(N)=NCCC[C@H](N)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		168293467	192151	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5203840	192151	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2480	82	30	32	-6.3	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	10.1021/acs.jmedchem.2c00786
		44393850	66097	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL183890	66097	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	589	10	3	6	2.9	CN(CCO)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44447821	167462	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C3CCC3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL429853	167462	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C3CCC3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44412681	138195	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccc(CC(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		CHEMBL376973	138195	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	626	12	3	7	3.0	COc1ccc(CC(=O)NCc2cccnc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)cc1	10.1016/j.bmcl.2006.04.069
		44444444	161889	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	494	6	0	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL415086	161889	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	494	6	0	4	4.7	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44447764	95542	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	552	7	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2(Cc3ccc(Cl)cc3)COC(=O)N2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257538	95542	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	552	7	2	5	4.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2(Cc3ccc(Cl)cc3)COC(=O)N2)CC1	10.1016/j.bmcl.2008.01.125
		44434772	88597	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235582	88597	0	None	-3	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	513	9	2	2	6.7	C=C(Br)CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		70688108	75071	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	418	8	4	4	1.7	O=C(CNC(=O)[C@H]1CNC[C@H]1C(=O)NCCc1c[nH]c2ccccc12)c1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035933	75071	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	418	8	4	4	1.7	O=C(CNC(=O)[C@H]1CNC[C@H]1C(=O)NCCc1c[nH]c2ccccc12)c1ccccc1	10.1016/j.bmc.2012.04.001
		70683847	75072	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	390	7	4	3	2.0	O=C(NCCc1c[nH]c2ccccc12)[C@@H]1CNC[C@@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035934	75072	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	390	7	4	3	2.0	O=C(NCCc1c[nH]c2ccccc12)[C@@H]1CNC[C@@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		25133903	170558	0	None	7	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
		CHEMBL445009	170558	0	None	7	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	596	11	3	6	3.1	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCNc2ccccn2)C1=O	10.1021/jm800525p
		5624	32693	14	None	-169	10	Human	4.3	pKi	=	4.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL1203324	32693	14	None	-169	10	Human	4.3	pKi	=	4.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		CHEMBL141343	32693	14	None	-169	10	Human	4.3	pKi	=	4.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL	520	5	1	8	4.2	Cc1c(C)c2c(c(C)c1O)CCC(C)(CN1CCN(c3cc(N4CCCC4)nc(N4CCCC4)n3)CC1)O2	nan
		44413881	137593	0	None	-1	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL375559	137593	0	None	-1	3	Human	6.3	pKi	=	6.3	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	707	15	6	7	1.9	CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		44433275	151707	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	647	14	1	5	6.0	CCN(CC)CCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396432	151707	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	647	14	1	5	6.0	CCN(CC)CCN[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44391391	64638	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccn2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL181788	64638	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	617	11	4	7	3.1	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)C(N)Cc2ccccn2)CC1	10.1016/j.bmcl.2004.10.096
		44415630	80031	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	4	5.9	CCC(C)[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212897	80031	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	558	10	2	4	5.9	CCC(C)[C@H](NCCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447772	95663	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)C3NCCC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL258036	95663	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	454	5	2	4	4.1	Cc1ccc(N2CCN(C(=O)C3NCCC3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		46885524	7804	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		CHEMBL1089462	7804	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		CHEMBL1204054	7804	0	None	-	1	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	458	5	1	5	3.6	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@H]2CN(c3cccnn3)C[C@@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		44562594	174155	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	503	9	1	4	5.5	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454670	174155	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	503	9	1	4	5.5	CC(C)CC(=O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44455957	155070	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	10	1	5	4.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL401792	155070	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	583	10	1	5	4.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cccc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44412691	138392	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	12	4	7	3.1	COc1ccccc1CNC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL377269	138392	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	12	4	7	3.1	COc1ccccc1CNC(=O)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		9842665	156806	12	None	-3	2	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44447771	155213	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	5	2	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL402587	155213	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	492	5	2	4	4.6	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44442956	94348	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL250701	94348	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	2	5	4.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ncc[nH]4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44434759	88516	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235139	88516	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434690	89306	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	89306	0	None	-4	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434714	148392	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL393753	148392	0	None	-1	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccccn3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44265591	172043	0	None	-1	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	499	12	7	4	2.3	N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(02)00089-6
		CHEMBL447178	172043	0	None	-1	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	499	12	7	4	2.3	N=C(N)NCCC[C@@H](NCc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(02)00089-6
		44265487	97383	0	None	-2	4	Human	4.3	pKi	=	4.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	256	6	4	2	1.8	N=C(N)NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL269689	97383	0	None	-2	4	Human	4.3	pKi	=	4.3	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	256	6	4	2	1.8	N=C(N)NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		44433292	152793	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	10	2	5	5.0	CC(C)C[C@H](NC(=O)C(C)(C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL397368	152793	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	633	10	2	5	5.0	CC(C)C[C@H](NC(=O)C(C)(C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44323020	168996	0	None	-7	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	951	11	12	9	1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL439188	168996	0	None	-7	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	951	11	12	9	1.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		10077594	75590	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		CHEMBL204670	75590	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	618	12	2	3	6.5	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCCN(C)Cc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		168290484	191854	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	5	1	7	3.9	Cc1nc2c(cc1-c1cnn(C)c1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5199107	191854	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	482	5	1	7	3.9	Cc1nc2c(cc1-c1cnn(C)c1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(OC(F)F)nc3)C1)N2	10.1021/acsmedchemlett.2c00229
		44415359	139546	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	511	8	1	4	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL379625	139546	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	511	8	1	4	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(OC)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		11845450	138469	0	None	-44	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL377465	138469	0	None	-44	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	652	15	5	6	2.6	CC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		11238126	165348	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL423619	165348	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	546	8	2	5	3.8	CCOc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44400770	133549	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	598	12	3	7	5.0	O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		CHEMBL370926	133549	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	598	12	3	7	5.0	O=C(N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)OCc1ccccc1	10.1016/j.bmcl.2005.03.053
		44415926	141382	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	453	7	1	3	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL383849	141382	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	453	7	1	3	5.8	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC2CCCCC2)CC1	10.1016/j.bmcl.2006.06.075
		44434872	88564	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		CHEMBL235382	88564	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	NC1CCCC(N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)C1	10.1016/j.bmc.2007.06.003
		44393430	124363	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	524	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL363757	124363	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	524	6	2	4	3.6	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CC[N+]([O-])(C2CCCCC2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL3646878	212017	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3646878	212017	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		44413577	139526	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL379531	139526	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	711	10	10	7	0.0	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		44347106	115060	0	None	46	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	738	9	10	7	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL334309	115060	0	None	46	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	738	9	10	7	0.1	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44323233	106716	0	None	4	2	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL314401	106716	0	None	4	2	Human	7.2	pKi	=	7.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	901	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)c2ccccc2C(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		11364326	66686	0	None	-27	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		CHEMBL185455	66686	0	None	-27	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		44433450	88485	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	502	7	2	5	3.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCO)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL234984	88485	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	502	7	2	5	3.5	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(CCO)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44444435	154845	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cnnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400510	154845	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	492	6	0	6	3.8	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3Cn3cnnc3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44562284	189039	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	601	16	0	4	8.2	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL509340	189039	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	601	16	0	4	8.2	CCCCCN(CCCCC)[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44434572	166592	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	9	2	2	4.6	NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL428022	166592	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	9	2	2	4.6	NCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		70690146	75070	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	433	8	3	3	2.9	O=C(NCc1ccc(C(F)(F)F)cc1)[C@@H]1CNC[C@@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035932	75070	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	433	8	3	3	2.9	O=C(NCc1ccc(C(F)(F)F)cc1)[C@@H]1CNC[C@@H]1C(=O)NCCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL5075506	214379	0	None	-457	3	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44433391	154931	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.6	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL401025	154931	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.6	CCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL438596	213781	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44447822	95551	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257584	95551	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	5	1	5	4.6	COC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44413938	138939	0	None	2	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL378446	138939	0	None	2	3	Human	7.2	pKi	=	7.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	662	15	4	5	3.9	CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		9958649	124357	0	None	-53	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
		CHEMBL363730	124357	0	None	-53	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	CC1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CC(C)N1	10.1021/jm0400496
		44447244	94547	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		CHEMBL251814	94547	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	455	5	1	4	4.7	Cc1ccc(N2CCN(C(=O)[C@@H]3CCO[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.11.128
		44415727	141781	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	10	1	3	8.2	CCC(C)[C@H](NCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL386123	141781	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	605	10	1	3	8.2	CCC(C)[C@H](NCc1ccccc1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44434666	88559	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	434	9	1	3	5.8	NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235356	88559	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	434	9	1	3	5.8	NCCCCCN(C(=O)COc1ccc2ccccc2c1)C1CCC2(CC=CCC2)CC1	10.1016/j.bmc.2007.06.003
		44434778	89743	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237702	89743	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	544	9	1	3	7.8	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)COc3ccc4ccccc4c3)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434654	90021	0	None	-21	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.4	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238134	90021	0	None	-21	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	421	10	2	2	5.4	NCCCCCN(C/C(Cl)=C\c1ccccc1)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44433286	169251	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.4	CNCC(=O)N[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL441136	169251	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	11	2	5	4.4	CNCC(=O)N[C@@H](CC(C)C)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44416060	81318	0	None	52	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL215895	81318	0	None	52	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	734	13	5	6	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2Cc3ccccc3CN2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		88565595	125065	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644355	125065	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644345	211984	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644351	211990	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3644358	211992	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](N)CN2C1=O	nan
		CHEMBL3646882	212021	0	None	19	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646891	212029	0	None	25	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88565595	125065	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		CHEMBL3644355	125065	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1095	19	17	12	-2.3	CCNC(=O)[C@@H]1CCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1	nan
		134134990	143906	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3901972	143906	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1042	16	16	12	0.7	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](N)CN2C1=O	nan
		CHEMBL3644345	211984	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644351	211990	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3646882	212021	0	None	19	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3646891	212029	0	None	25	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3663352	212082	0	None	63	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H]([C@@H](C)O)NC1=O	nan
		CHEMBL3663358	212088	0	None	69	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](C(C)C)NC1=O	nan
		CHEMBL3663381	212110	0	None	15	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667929	212123	0	None	43	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667956	212150	0	None	23	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		10030530	17599	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		CHEMBL125819	17599	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counterDisplacement of 125I-NDP-a-MSH from human Melanocortin receptor 4 after 2 hrs by TopCount microplate scintillation and luminescence counter	ChEMBL	552	10	1	4	4.8	CCN(C(C)=O)C(C)c1ccccc1N1CCN(C(=O)[C@H](CC(=O)NC2CCC2)Cc2ccc(Cl)cc2)CC1	10.1021/acs.jmedchem.5b00982
		CHEMBL2415083	210434	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCCCn1cc(CCCCOC(CCC(O)C(C)CCC(O)C(C)CCC(O)C(C)C)C(C)CCC(O)C(C)CCC(O)C(C)C)nn1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1016/j.bmc.2013.06.052
		44434558	89492	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237266	89492	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		23635106	91557	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		23635106	91557	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		CHEMBL240568	91557	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1016/j.bmc.2008.03.072
		CHEMBL240568	91557	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	502	10	2	4	4.8	CNCCN[C@H](c1cc(C)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1)C(C)C	10.1021/jm070806a
		24740312	89372	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236979	89372	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	519	9	2	5	4.1	CC(C)C[C@@H](NC(=O)CN)c1cccnc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		25129105	177019	0	None	23	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
		CHEMBL463047	177019	0	None	23	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	623	11	2	5	3.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)c1cccnc1	10.1021/jm800525p
		25129109	188702	0	None	16	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
		CHEMBL504349	188702	0	None	16	3	Human	8.2	pKi	=	8.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	12	3	5	2.8	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)NC	10.1021/jm800525p
		44412513	159414	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL410087	159414	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	657	12	2	6	4.2	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		44433265	146076	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	576	10	1	4	5.7	CCN[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL391915	146076	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	576	10	1	4	5.7	CCN[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		6918847	176972	1	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	526	9	2	6	2.6	CCOC(=O)[C@H]1CCCC[C@@H]1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462380	176972	1	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	526	9	2	6	2.6	CCOC(=O)[C@H]1CCCC[C@@H]1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		11490658	64943	0	None	301	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL182277	64943	0	None	301	2	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	642	10	4	6	4.4	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2004.10.096
		122178162	121256	0	None	-	1	Mouse	8.2	pKi	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577991	121256	0	None	-	1	Mouse	8.2	pKi	=	8.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	991	13	10	10	-0.8	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(CCc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		44433267	89464	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	592	11	2	5	4.7	CC(C)C[C@H](NCCO)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237147	89464	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	592	11	2	5	4.7	CC(C)C[C@H](NCCO)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44433262	146073	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL391914	146073	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11296600	122943	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL360716	122943	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		11296600	122943	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL360716	122943	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44433262	146073	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL391914	146073	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	530	8	1	4	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		10283067	76527	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL206042	76527	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	649	12	2	5	5.5	CCN(CC)CC(c1ccccc1Cl)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		11296600	122943	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		CHEMBL360716	122943	0	None	41	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	628	9	4	6	3.8	CC(NC1CCCNC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm049278i
		44397198	66765	0	None	93	3	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells; Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells;	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL185862	66765	0	None	93	3	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells; Inhibition of [125I]-AgRP(83132) (radioligand) binding to the hMC4R stably expressed in HEK293 cells;	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44432933	86793	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232164	86793	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44416197	165978	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL425261	165978	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	525	8	1	4	5.9	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44432933	86793	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232164	86793	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	560	14	2	6	6.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(C(N)=O)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44447804	155594	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL404503	155594	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44433426	169024	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	6.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCCCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL439387	169024	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	6.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCCCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL264132	210606	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H]1CSSC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cncn2C)NC(=O)[C@@H](CCC(=O)O)NC1=O	10.1021/jm0501432
		16038315	138758	0	None	309	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	13	3	7	3.5	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL378046	138758	0	None	309	3	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	612	13	3	7	3.5	COc1ccccc1CCNCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		1338	3807	43	None	53	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		24886259	11826	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	619	9	2	5	5.2	CN1CCC(CC2CCCCC2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182116	11826	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	619	9	2	5	5.2	CN1CCC(CC2CCCCC2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL213340	11826	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	619	9	2	5	5.2	CN1CCC(CC2CCCCC2)(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CC1	10.1016/j.bmcl.2006.04.016
		168271899	190601	0	None	3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3020	70	35	39	-5.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5180727	190601	0	None	3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3020	70	35	39	-5.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433269	89538	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237364	89538	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	591	11	2	5	4.7	CC(C)C[C@H](NCCN)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		11226756	119974	0	None	23	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL349850	119974	0	None	23	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	559	8	2	5	3.5	CN(C)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL3644322	211962	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		CHEMBL3644322	211962	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O	nan
		44405395	135262	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	10	2	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cccnc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL372576	135262	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	601	10	2	5	4.3	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cccnc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44416160	81324	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	513	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215905	81324	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	513	7	1	3	6.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		44432898	87026	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232532	87026	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		44397280	67303	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	13	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL188341	67303	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	13	3	5	4.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCCCc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168286369	191712	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2962	64	33	37	-4.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5197030	191712	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2962	64	33	37	-4.5	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44432898	87026	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL232532	87026	1	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	491	13	2	6	5.9	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		44347379	114436	0	None	4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	750	9	9	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL333263	114436	0	None	4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	750	9	9	7	0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NC2CCC(C(N)=O)N2C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44395436	66859	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186239	66859	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	482	9	2	5	4.0	N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL2415017	210428	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGOMSH(7) from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(O)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)CCC(O)C(C)CCC(O)C(C)C	10.1016/j.bmc.2013.06.052
		9852314	79032	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113137	79032	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	2.7	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44434690	89306	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL236861	89306	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	NC1CCC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434821	90028	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	441	10	4	2	4.5	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238149	90028	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	441	10	4	2	4.5	N=C(N)NCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44455958	155071	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL401793	155071	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	651	10	1	5	5.5	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(C(F)(F)F)cc2F)CC1	10.1016/j.bmcl.2007.10.115
		44405382	132828	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	651	10	2	5	5.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cnc4ccccc4c3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL370178	132828	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	651	10	2	5	5.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3cnc4ccccc4c3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44397121	123427	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL361719	123427	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	591	11	3	5	4.1	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNCc3ccc(F)cc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		168271934	190085	0	None	-34	3	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5172738	190085	0	None	-34	3	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2229	37	32	26	-3.7	C#CCCCCN1C(=O)C2=C(SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2c[nH]c4ccccc24)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC3=O)C1=O	10.1021/acs.jmedchem.2c00793
		44433564	96459	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	632	7	1	4	7.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL262319	96459	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	632	7	1	4	7.2	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(Cc3ccccc3)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		44415809	81491	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	10	1	6	5.1	COc1cc(OC)c(OC)cc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL216009	81491	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	537	10	1	6	5.1	COc1cc(OC)c(OC)cc1CCC(=O)N1CCN(c2ccc(C(F)(F)F)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.05.088
		137638725	156979	0	None	-1	2	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4073016	156979	0	None	-1	2	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		137659790	159322	0	None	-5	3	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		CHEMBL4099889	159322	0	None	-5	3	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		137636965	156216	0	None	-5	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4064433	156216	0	None	-5	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1742	21	20	21	-2.9	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL438030	213744	0	None	-1	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O	10.1021/jm030119t
		44447819	155420	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.7	CCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL403699	155420	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	510	6	1	4	4.7	CCC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44443016	94088	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		CHEMBL249064	94088	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	566	9	1	5	5.4	COc1ccccc1CNCC1(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@@H]3c3ccc(Cl)cc3)CC2)CCCCC1	10.1016/j.bmcl.2007.10.032
		46885415	8279	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1092571	8279	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	468	4	1	3	4.5	C[C@H]1CN(C(=O)[C@H]2CN(C3CCC3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44397225	168218	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	645	11	4	6	4.1	CN(C)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL433555	168218	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	645	11	4	6	4.1	CN(C)c1ccc(NC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		44415442	138924	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	11	1	4	6.6	COCCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL378397	138924	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	573	11	1	4	6.6	COCCN[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44348151	113968	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	428	5	0	3	5.6	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		CHEMBL332602	113968	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	428	5	0	3	5.6	COc1ccc(Br)cc1CCc1c(F)cccc1-c1ncc2n1CCCC2	10.1016/j.bmcl.2004.05.003
		10134057	88657	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	8	2	3	3.6	C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235815	88657	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	8	2	3	3.6	C/C(=C\c1ccccc1)CN(CCCN)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434636	89300	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	469	12	3	3	5.6	NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236841	89300	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	469	12	3	3	5.6	NCCCCN(Cc1ccccc1)C(=O)CCCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		70690148	75084	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	464	10	3	5	1.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCO)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035946	75084	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	464	10	3	5	1.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CCO)C[C@@H]1C(=O)NCCc1ccccc1	10.1016/j.bmc.2012.04.001
		10158674	147915	0	None	-8	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.4	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393359	147915	0	None	-8	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.4	NCCCCCN(Cc1ccc2ccccc2c1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		25131477	178701	0	None	27	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
		CHEMBL468252	178701	0	None	27	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	547	10	2	5	2.2	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCN(C)C)C1=O	10.1021/jm800525p
		88944403	147277	0	None	-6309	2	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	979	16	13	10	-0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3928766	147277	0	None	-6309	2	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	979	16	13	10	-0.2	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		122178165	121259	0	None	-	1	Mouse	7.2	pKi	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577994	121259	0	None	-	1	Mouse	7.2	pKi	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL	1027	12	10	10	-0.1	C[C@@H]1NC(=O)[C@H](CC(N)=O)NC(=O)C(Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O	10.1021/acs.jmedchem.5b00184
		CHEMBL3577978	211746	0	None	10	2	Mouse	7.2	pKi	=	7.2	Binding	Displacement of MTII from mouse MC4R expressed in HEK293 cellsDisplacement of MTII from mouse MC4R expressed in HEK293 cells	ChEMBL		None	None	None		CC(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CSSC[C@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N2)[C@@H](C)O	10.1021/acs.jmedchem.5b00184
		10260053	168203	0	None	-4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		CHEMBL433413	168203	0	None	-4	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	871	27	12	10	-1.1	NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCC(=O)O)C(N)=O	10.1021/jm020021z
		11237928	164871	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL422027	164871	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	532	7	3	5	2.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CO)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		44432897	147625	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393133	147625	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		10053261	140546	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	548	12	2	4	5.2	CCN(CC)CCCC(C)/N=C(/NC)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL381085	140546	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	548	12	2	4	5.2	CCN(CC)CCCC(C)/N=C(/NC)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		137646617	157544	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4080223	157544	0	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1728	21	21	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44413913	138673	0	None	1	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		CHEMBL377779	138673	0	None	1	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	672	16	6	7	0.2	CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1C(=O)NCCN=C(N)N	10.1021/jm060384p
		11756904	76586	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
		CHEMBL206316	76586	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	533	9	2	4	3.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCN1CCN(C)CC1	10.1016/j.bmcl.2006.01.016
		88590620	125062	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644352	125062	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		88590620	125062	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644352	125062	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1098	20	17	12	-2.9	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)NC2CC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667931	212125	0	None	154	2	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		44433424	146563	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	8	1	5	4.7	COCC(C)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL392287	146563	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	526	8	1	5	4.7	COCC(C)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44415692	80324	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL214217	80324	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	598	10	2	4	6.7	CCC(C)[C@H](NC[C@@H]1CCCN1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		46885558	7809	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089483	7809	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	492	4	1	5	4.0	C[C@H]1CN(C(=O)[C@H]2CN(c3ccncn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL5094168	215479	0	None	-436	3	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		11387898	56048	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL162493	56048	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	608	9	2	5	5.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2OCc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		11353851	57472	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL165746	57472	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	594	8	2	5	5.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2Oc2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		88944280	145084	0	None	-213	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	922	15	13	10	-1.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3911582	145084	0	None	-213	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	922	15	13	10	-1.7	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)C2CC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		44415747	141481	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	486	7	2	3	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c[nH]c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL384389	141481	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	486	7	2	3	5.5	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2c[nH]c3ccccc23)CC1	10.1016/j.bmcl.2006.05.088
		44432897	147625	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL393133	147625	1	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	539	17	2	8	6.0	CCCCCN(CCCCC)C(=O)c1ccc2nc(Nc3cc(OC)c(OC)c(OC)c3)n(CCCN)c2c1	10.1016/j.bmcl.2007.06.010
		44395503	66956	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	496	10	2	5	4.2	NCC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186696	66956	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	496	10	2	5	4.2	NCC(Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		44434662	88514	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.6	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235137	88514	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.6	NCCCCCN(Cc1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434754	90236	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238345	90236	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434601	146468	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	8	1	2	4.3	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		CHEMBL392223	146468	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	358	8	1	2	4.3	NCCCN(C/C=C/c1ccccc1)C(=O)Cc1ccc2ccccc2c1	10.1016/j.bmc.2007.06.003
		9969456	147617	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	7	2	2	4.7	NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393125	147617	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	371	7	2	2	4.7	NCCCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265711	206989	0	None	-4	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	343	6	3	2	3.5	NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		CHEMBL9138	206989	0	None	-4	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	343	6	3	2	3.5	NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00089-6
		1338	3807	43	None	53	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		9938402	3807	43	None	53	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL339053	3807	43	None	53	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from MC4R D122A mutant expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL3667952	212146	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(=O)O)NC1=O	nan
		CHEMBL3667951	212145	0	None	15	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)[C@H](CC(=O)O)NC1=O	nan
		44401275	69034	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	647	12	5	5	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(C(=O)c2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL192354	69034	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	647	12	5	5	2.8	N=C(N)NCCC[C@H](NC(=O)Cc1ccc2ccccc2c1)C(=O)N1CCN(C(=O)c2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44562289	188959	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL508284	188959	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	9	3	5	3.7	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)[C@@H](C)N)CC1	10.1016/j.bmcl.2008.07.076
		44433411	166961	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	614	10	1	4	6.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL428731	166961	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	614	10	1	4	6.6	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCCCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44443027	155020	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL401488	155020	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	579	9	1	5	5.5	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(N(C)C)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11341045	66166	0	None	-36	4	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
		CHEMBL184275	66166	0	None	-36	4	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	501	6	3	3	5.0	O=C(NCCc1ccc(Cl)cc1Cl)c1ccc(N/C(=N/C2CCCCC2)N2CCNCC2)cc1	10.1021/jm0400496
		44434868	149551	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	635	11	5	4	6.7	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		CHEMBL394669	149551	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	635	11	5	4	6.7	NC1CCCC(NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c(Cc4ccc(O)cc4)[nH]c4ccccc34)C2)C1	10.1016/j.bmc.2007.06.003
		44562538	174376	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1ccccc1CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL455188	174376	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1ccccc1CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44562539	174378	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1cccc(CC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)c1	10.1016/j.bmcl.2008.07.076
		CHEMBL455189	174378	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	598	11	3	6	4.0	COc1cccc(CC(O)c2ccccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3Cl)NC(=O)CCN)CC2)c1	10.1016/j.bmcl.2008.07.076
		44395647	123106	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	11	3	6	3.8	CC(C)(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL361074	123106	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	567	11	3	6	3.8	CC(C)(N)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644334	211974	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		134144957	150683	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1059	19	17	12	2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCC(N)=O)/N=C\1O	nan
		CHEMBL3955830	150683	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1059	19	17	12	2.0	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1CC/C(O)=N\CCC[C@H](C(=O)O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@@H](CCC(N)=O)/N=C\1O	nan
		44394010	125425	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL364577	125425	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	599	9	3	5	4.5	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CCCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44433380	88487	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL234992	88487	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	564	6	1	4	5.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL91957	215905	0	None	2	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL		None	None	None		N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NS(=O)(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		11375529	120151	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		CHEMBL351400	120151	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	502	6	2	4	3.4	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2)CC1)[C@H]1Cc2ccccc2CN1	10.1021/jm0304109
		70688109	75076	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	399	6	3	3	3.4	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)Nc1cccc(-c2ccccc2)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035938	75076	0	None	-	1	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	399	6	3	3	3.4	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)Nc1cccc(-c2ccccc2)c1	10.1016/j.bmc.2012.04.001
		44265658	10180	0	None	-14	2	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	314	8	4	3	1.4	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)O	10.1016/s0960-894x(02)00089-6
		CHEMBL1159698	10180	0	None	-14	2	Human	4.2	pKi	=	4.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	314	8	4	3	1.4	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)O	10.1016/s0960-894x(02)00089-6
		10132207	88651	0	None	-18	3	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	343	5	2	2	3.9	NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235797	88651	0	None	-18	3	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	343	5	2	2	3.9	NCCN(Cc1ccc2ccccc2c1)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44413970	139015	0	None	-14	3	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL378571	139015	0	None	-14	3	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		44401418	124016	0	None	2	2	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	621	14	6	4	3.3	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL362964	124016	0	None	2	2	Human	6.2	pKi	=	6.2	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	621	14	6	4	3.3	N=C(N)NCCC[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCCc1ccccc1	10.1016/j.bmcl.2005.03.120
		44433388	88572	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
		CHEMBL235432	88572	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	560	8	1	5	5.5	COc1ccc([C@@H]2CN(C(C)C)C[C@H]2C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)cc1	10.1016/j.bmcl.2007.09.079
		44416200	81325	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215906	81325	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	445	7	1	3	5.1	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2F)CC1	10.1016/j.bmcl.2006.06.075
		44416162	141589	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL385003	141589	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	461	7	1	3	5.6	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		168283984	191246	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2937	64	35	39	-7.9	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5190172	191246	0	None	3	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2937	64	35	39	-7.9	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44322869	106160	0	None	-6	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL313690	106160	0	None	-6	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	867	11	12	9	-0.4	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44413537	139547	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		CHEMBL379627	139547	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human cloned MC4R expressed in HEK293 cells	ChEMBL	739	10	10	7	0.8	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)CCCCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O	10.1016/j.bmcl.2006.04.050
		70688110	75078	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		CHEMBL2035940	75078	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	508	10	2	4	3.3	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCCc1cccc(Cl)c1	10.1016/j.bmc.2012.04.001
		44443007	153839	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	4.5	CC(C)C(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL398266	153839	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	593	9	2	5	4.5	CC(C)C(N)C(=O)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44413831	78064	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL210008	78064	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		44347990	15726	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	6	0	3	6.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C(C)C	10.1016/j.bmcl.2004.05.003
		CHEMBL122253	15726	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	432	6	0	3	6.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1-c1nccn1C(C)C	10.1016/j.bmcl.2004.05.003
		44453902	95434	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	391	10	5	3	2.4	N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		CHEMBL257040	95434	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	391	10	5	3	2.4	N=C(N)NCCC[C@H](CC1CCCCC1)NC(=O)[C@H](N)Cc1ccc(F)cc1	10.1016/j.bmcl.2007.11.109
		10155513	151541	0	None	-7	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	2	4.0	C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL396303	151541	0	None	-7	4	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	8	2	2	4.0	C/C(=C\c1ccccc1)CN(CCCN)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44322895	163370	0	None	-11	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL419307	163370	0	None	-11	3	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	811	21	10	8	1.3	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)COc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44433392	88573	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.0	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		CHEMBL235433	88573	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	524	7	1	4	5.0	CCCC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](N)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.09.079
		44447824	155504	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL404141	155504	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	5	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)OC(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44413666	11823	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	582	9	2	5	5.1	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCSCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182095	11823	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	582	9	2	5	5.1	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCSCC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211475	11823	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	582	9	2	5	5.1	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCSCC1	10.1016/j.bmcl.2006.04.016
		88878645	145819	0	None	-22387	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1053	19	15	12	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3917089	145819	0	None	-22387	2	Human	6.2	pKi	=	6.2	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1053	19	15	12	-2.7	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44265639	10179	0	None	-5	4	Human	5.2	pKi	=	5.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL1159697	10179	0	None	-5	4	Human	5.2	pKi	=	5.2	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	439	9	4	3	4.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)Nc1cccc2ccccc12	10.1016/s0960-894x(02)00089-6
		44434690	89905	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237920	89905	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	545	10	2	2	8.1	N[C@H]1CC[C@H](C[C@H]2CC[C@H](N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		10178845	89914	0	None	-6	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	8	2	3	3.8	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237937	89914	0	None	-6	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	395	8	2	3	3.8	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265479	206089	0	None	1	2	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	268	2	2	2	1.9	N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1	10.1016/s0960-894x(02)00088-4
		CHEMBL8561	206089	0	None	1	2	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	268	2	2	2	1.9	N=C(N)N1CCN(Cc2ccc3ccccc3c2)CC1	10.1016/s0960-894x(02)00088-4
		23635105	154979	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23635105	154979	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		CHEMBL401250	154979	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL401250	154979	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	427	6	1	3	4.8	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		11468019	66984	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		CHEMBL186841	66984	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1021/jm049278i
		44413602	11819	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCCCCCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182085	11819	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCCCCCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL210922	11819	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	607	12	2	5	5.2	CCCCCCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCN(C)CC1	10.1016/j.bmcl.2006.04.016
		44410385	139854	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
		CHEMBL379918	139854	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1ccc2ccccc2c1	10.1016/j.bmcl.2006.01.016
		44415429	80027	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	467	8	1	4	4.5	CCOCC(N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL212889	80027	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	467	8	1	4	4.5	CCOCC(N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44442989	93886	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	9	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL248028	93886	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	9	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44348039	16424	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cn(C)c(-c2ccccc2CCc2cc(Br)ccc2OC)n1	10.1016/j.bmcl.2004.05.003
		CHEMBL123149	16424	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	398	6	0	3	5.2	CCc1cn(C)c(-c2ccccc2CCc2cc(Br)ccc2OC)n1	10.1016/j.bmcl.2004.05.003
		137646333	157922	0	None	-4	2	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4084386	157922	0	None	-4	2	Human	4.2	pKi	=	4.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1756	21	19	21	-2.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)N(C)C(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44433289	151712	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396434	151712	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	619	10	2	5	4.6	CC(C)C[C@H](NC(=O)[C@@H](C)N)c1cc(F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		44415912	139226	0	None	10	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL378837	139226	0	None	10	3	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human MC4RBinding affinity to human MC4R	ChEMBL	575	11	4	5	1.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](CCCN=C(N)N)C1=O	10.1016/j.bmcl.2006.05.087
		CHEMBL3644317	211957	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644326	211966	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646879	212018	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644317	211957	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644326	211966	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646879	212018	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3663350	212080	0	None	18	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663374	212103	0	None	8	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667926	212120	0	None	245	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3667930	212124	0	None	34	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667950	212144	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2CCCN2C1=O	nan
		CHEMBL3667958	212152	0	None	36	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667961	212155	0	None	53	2	Human	8.2	pKi	=	8.2	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		136024005	87301	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233176	87301	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44412758	166039	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	641	10	1	6	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)n2cc3ccccc3c2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL425609	166039	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	641	10	1	6	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)n2cc3ccccc3c2)CC1)S(C)(=O)=O	10.1016/j.bmcl.2006.04.002
		136024005	87301	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL233176	87301	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	541	12	1	4	7.6	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(-c3c[nH]c4ccccc34)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44434560	89494	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL237268	89494	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	537	9	3	5	3.5	CC(C)C[C@@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmc.2007.05.026
		44444493	155130	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		CHEMBL402058	155130	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	581	9	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.06.088
		44456410	97439	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL270015	97439	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	553	9	2	5	4.1	Cc1ccc(N2CCN(C(=O)[C@@H]3CNC[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		44447779	95043	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL255099	95043	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44432928	167643	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL430165	167643	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44322896	167972	0	None	1	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL431801	167972	0	None	1	2	Human	8.1	pKi	=	8.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	789	22	10	7	1.6	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CCCc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44456138	95353	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL256686	95353	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	609	8	2	6	4.4	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C4CCOCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)[C@@H](C)N)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		10232787	140381	0	None	165	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL380855	140381	0	None	165	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	619	12	2	5	5.0	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		44432928	167643	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL430165	167643	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	517	13	1	5	7.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccccc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44447804	155594	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL404503	155594	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	525	5	1	4	4.5	Cc1ccc(N2CCN(C(=O)[C@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)N(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44434557	145449	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL391427	145449	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	522	8	2	4	4.6	CC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2c(F)cccc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmc.2007.05.026
		44455922	155136	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL402075	155136	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	633	10	1	5	5.7	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.10.115
		44577060	188052	0	None	-2	8	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL497746	188052	0	None	-2	8	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	530	10	1	4	4.8	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		44432947	86996	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232387	86996	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44432947	86996	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232387	86996	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	595	13	1	5	8.0	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Br)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44456336	156098	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		CHEMBL406309	156098	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	9	1	5	4.3	CC(=O)N1C[C@@H](C(=O)N2CCN(c3ccc(C)cc3[C@@H](NC(=O)CCN(C)C)C(C)C)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.10.115
		44397028	124031	0	None	61	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1	10.1016/j.bmcl.2005.05.017
		CHEMBL363019	124031	0	None	61	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	631	12	3	6	3.6	COc1cccc(CC(=O)NCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)c1	10.1016/j.bmcl.2005.05.017
		44562478	194103	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	9	3	5	4.2	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL528108	194103	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	9	3	5	4.2	CC(C)CC(N)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)C(C)(C)N)CC1	10.1016/j.bmcl.2008.07.076
		44444504	154917	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL400934	154917	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.6	CNCC(=O)N[C@@H](CC(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL2070373	209186	0	None	14	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbuminDisplacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)COCCOCCNC(=O)CCCCCCCCCCCCCCCc1nnn[nH]1)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C1=O	10.1021/jm201489a
		44433266	89463	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	604	11	0	4	6.4	CCN(CC)[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL237146	89463	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	604	11	0	4	6.4	CCN(CC)[C@@H](CC(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		10098971	124024	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL362985	124024	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	546	11	0	5	5.7	COc1ccc2ccccc2c1CCCCN1CCN(CC(c2ccc(F)cc2)N2CCN(C(C)C)CC2)CC1	10.1016/j.bmcl.2005.03.053
		44432906	148898	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL394167	148898	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL5076315	214428	0	None	1	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44432906	148898	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		CHEMBL394167	148898	1	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	16	1	6	7.2	CCN(CC)CCCn1c(Nc2ccc(C(C)=O)cc2)nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc21	10.1016/j.bmcl.2007.06.010
		11468019	66984	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186841	66984	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	554	12	2	6	3.8	COCC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2004.08.055
		60168008	75082	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	528	9	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		CHEMBL2035944	75082	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	528	9	2	4	4.0	O=C(NC1CCN(Cc2ccccc2)C1)[C@@H]1CN(CC2CC2)C[C@@H]1C(=O)NCc1ccc(Cl)cc1Cl	10.1016/j.bmc.2012.04.001
		44404568	72298	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	309	6	0	3	3.0	CCN(CC)CC(c1ccccc1Cl)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198320	72298	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	309	6	0	3	3.0	CCN(CC)CC(c1ccccc1Cl)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		44404570	72316	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	6	0	3	2.6	CCN(CC)CC(c1ccccc1C)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL198378	72316	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	289	6	0	3	2.6	CCN(CC)CC(c1ccccc1C)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		58777892	79044	0	None	4	4	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113149	79044	0	None	4	4	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)C1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		24886735	79731	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	579	10	2	5	3.9	CCN(CC)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCC1	10.1016/j.bmcl.2006.04.002
		CHEMBL211616	79731	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	579	10	2	5	3.9	CCN(CC)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)CCCC1	10.1016/j.bmcl.2006.04.002
		44410207	161759	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
		CHEMBL413931	161759	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	409	5	2	2	3.3	COc1ccc(Br)cc1CCc1c(Cl)cccc1C(=O)N=C(N)N	10.1016/j.bmcl.2006.01.016
		14364677	70631	2	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	204	2	0	2	2.0	CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL195009	70631	2	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	204	2	0	2	2.0	CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		71452733	79037	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113142	79037	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	585	7	2	5	3.8	CCN1CCc2c(cccc2N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@H]3Cc4ccccc4CN3)CC2)C1	10.1016/j.bmcl.2005.07.035
		44434759	88516	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL235139	88516	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	486	9	2	3	6.4	NC1CCC(CC2CCC(N(Cc3ccncc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434603	89913	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	409	10	2	2	4.9	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237935	89913	0	None	-1	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	409	10	2	2	4.9	NCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10292876	147954	0	None	-1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	7	2	2	3.8	NCCCN(C(=O)CCc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL393387	147954	0	None	-1	2	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	375	7	2	2	3.8	NCCCN(C(=O)CCc1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		71461662	79116	0	None	-6	4	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	442	9	4	3	3.2	NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL2113280	79116	0	None	-6	4	Human	4.2	pKi	=	4.2	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	442	9	4	3	3.2	NC(N)=NCCC[C@H](N)C(=O)N(Cc1cccc2ccccc12)Cc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00088-4
		137640703	157097	0	None	-54	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4074479	157097	0	None	-54	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44447227	154888	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL400786	154888	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	622	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44416194	80612	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		CHEMBL215106	80612	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	7	1	3	6.2	Cc1cc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)ccc1Cl	10.1016/j.bmcl.2006.06.075
		44412963	77367	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	4	7	2.0	CCC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208552	77367	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	4	7	2.0	CCC(CO)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44413056	79881	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	597	10	4	6	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL212325	79881	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	597	10	4	6	3.4	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)Nc2ccccc2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL438596	213781	0	None	-	1	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		156010247	177072	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	2913	40	44	46	-16.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.0c00485
		CHEMBL4633001	177072	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta countingDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO-K1 cell membranes incubated for 3 hrs by top-count beta counting	ChEMBL	2913	40	44	46	-16.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]2CSSC[C@@H]3NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc4cnc[nH]4)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N2)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC3=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.0c00485
		44434634	89299	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	1	5	6.5	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL236840	89299	0	None	-3	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	1	5	6.5	COc1ccc2c(c1)c(CC(=O)N(CCCCN)C/C(C)=C/c1ccccc1)c(C)n2C(=O)c1ccc(Cl)cc1	10.1016/j.bmc.2007.06.003
		44434651	89900	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	495	13	3	3	6.1	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237911	89900	0	None	-2	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	495	13	3	3	6.1	NCCCCCN(C/C=C\c1ccccc1)C(=O)CCc1c(Cc2ccc(O)cc2)[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		25132525	176725	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
		CHEMBL460142	176725	0	None	2	3	Human	6.2	pKi	=	6.2	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	8	2	4	2.9	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C(C)C)C1=O	10.1021/jm800525p
		168296741	192271	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5205686	192271	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5094215	215481	0	None	-6	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		11295737	120213	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		CHEMBL352063	120213	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cellsBinding affinity towards human melanocortin 4 receptor using [125I]NDP-alpha-MSH as a radioligand in HEK293 cells	ChEMBL	544	7	2	4	4.6	CC(C)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1021/jm0304109
		44432916	87557	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233544	87557	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		10211466	168900	0	None	19	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.1	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL438432	168900	0	None	19	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	633	12	2	5	5.1	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2(C)NCc3ccccc32)CC1	10.1016/j.bmcl.2005.10.103
		1334	1501	7	None	-1	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		None	10.1021/jm030119t
		16133814	1501	7	None	-1	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		None	10.1021/jm030119t
		CHEMBL437050	1501	7	None	-1	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		None	10.1021/jm030119t
		44432916	87557	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL233544	87557	1	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	547	14	1	6	7.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CC(C)(C)CN(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44434851	89909	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	10	2	2	5.7	NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		CHEMBL237930	89909	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	437	10	2	2	5.7	NCc1ccc(CN(C/C=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)cc1	10.1016/j.bmc.2007.06.003
		44434864	90249	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238369	90249	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	529	9	4	3	5.4	N[C@H]1CC[C@H](NC(=O)NC2CCCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C2)CC1	10.1016/j.bmc.2007.06.003
		88878672	153599	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	952	21	14	12	-3.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3980632	153599	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	952	21	14	12	-3.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44415406	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL213738	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.11.128
		44415406	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL213738	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.01.125
		44415406	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL213738	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2008.07.076
		44433561	145512	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL391481	145512	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	501	6	1	3	5.9	CC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2007.09.079
		44415406	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213738	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447234	94918	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254276	94918	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447802	95748	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	6	1	5	4.8	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(F)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL258412	95748	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	530	6	1	5	4.8	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccc(F)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		10291370	145966	0	None	-8	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	7	2	2	4.1	C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL391823	145966	0	None	-8	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	7	2	2	4.1	C/C(=C\c1ccccc1)CN(CCCN)C(=O)c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434787	148792	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	729	13	3	5	9.1	COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL394075	148792	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	729	13	3	5	9.1	COc1cc(Br)c(CN(C(=O)CCCc2c(Cc3ccc(O)cc3)[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434687	159492	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	465	14	2	2	6.5	NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL410179	159492	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	465	14	2	2	6.5	NCCCCCCCN(C/C(Cl)=C/c1ccccc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10269187	90116	0	None	-15	3	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.5	NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		CHEMBL238180	90116	0	None	-15	3	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	347	5	2	2	3.5	NCCCN(C(=O)c1c[nH]c2ccccc12)C1CCc2ccccc2C1	10.1016/j.bmc.2007.06.003
		137631599	156526	0	None	-109	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4067967	156526	0	None	-109	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1694	20	20	21	-3.2	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N(C)[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		70660693	151789	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	894	17	13	11	-3.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3965058	151789	0	None	-3715	2	Human	5.1	pKi	=	5.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	894	17	13	11	-3.1	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44396036	168343	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL434345	168343	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	593	11	3	6	4.3	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1)C1CCCCN1	10.1016/j.bmcl.2004.08.055
		CHEMBL3663324	212056	0	None	-5	2	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCN)NC1=O	nan
		168296741	192271	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5205686	192271	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3015	96	36	38	-7.6	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		44433407	152210	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	586	8	1	4	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL396866	152210	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	586	8	1	4	5.8	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)CCc4ccccc4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44415405	80213	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC[C@H](C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213691	80213	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC[C@H](C)C(N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44415406	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL213738	80226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	515	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44442941	152725	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL397312	152725	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	526	8	1	5	5.0	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccoc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		24886501	11824	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	614	9	2	6	3.7	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCS(=O)(=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL1182101	11824	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	614	9	2	6	3.7	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCS(=O)(=O)CC1	10.1016/j.bmcl.2006.04.016
		CHEMBL211792	11824	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from human MC4 receptor transfected in HEK293 cells	ChEMBL	614	9	2	6	3.7	CC(C)CC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)CC3NCc4ccccc43)CC2)CCS(=O)(=O)CC1	10.1016/j.bmcl.2006.04.016
		44405526	72409	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		CHEMBL198723	72409	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	594	10	2	4	5.0	CC(C)(C)CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.08.061
		44412990	77449	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	4	7	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208694	77449	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	617	11	4	7	3.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ncccc2CNC(=O)NCc2cccs2)CC1	10.1016/j.bmcl.2006.04.069
		44443041	154905	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	0	5	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN(C)Cc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400870	154905	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	551	8	0	5	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CN(C)Cc4ccncc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		168272615	190387	0	None	-6	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5177494	190387	0	None	-6	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1319	15	14	15	0.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](NC(C)=O)CSCc2ccc(cc2)CSC[C@@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44409206	140184	0	None	-1	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		CHEMBL380437	140184	0	None	-1	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	567	13	4	4	4.8	N=C(N)NCCC[C@H]1C[C@@H](OCc2ccccc2)CN1C(=O)[C@H](CC[C@H]1Cc2ccccc2CN1)Cc1ccccc1	10.1016/j.bmcl.2005.12.005
		44442977	93814	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL247636	93814	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	537	8	1	5	4.8	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccccn4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		25133907	176724	0	None	9	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		CHEMBL460138	176724	0	None	9	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	518	9	2	4	3.0	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@H](N)Cc1ccc(F)cc1	10.1021/jm800525p
		44413880	77946	0	None	-50	3	Human	6.1	pKi	=	6.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
		CHEMBL209587	77946	0	None	-50	3	Human	6.1	pKi	=	6.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	639	14	6	7	0.7	NC(N)=NCCNC(=O)[C@H]1C[C@@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1	10.1021/jm060384p
		11308184	64899	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL182231	64899	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	636	10	2	6	4.5	CN(Cc1cccnc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44432958	87209	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232775	87209	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		10049407	77330	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
		CHEMBL208366	77330	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	7	2	2	4.1	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCC(C)C	10.1016/j.bmcl.2006.01.016
		44433158	154932	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	463	11	2	6	5.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL401027	154932	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	463	11	2	6	5.1	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CC(C)C)CC(C)C)cc3n2CCCN)cc1	10.1016/j.bmcl.2007.06.010
		44434848	88968	0	None	-5	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		CHEMBL236443	88968	0	None	-5	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	461	9	2	2	6.3	NCc1cccc(CN(Cc2ccc3ccccc3c2)C(=O)CCCc2c[nH]c3ccccc23)c1	10.1016/j.bmc.2007.06.003
		44434854	90029	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		CHEMBL238153	90029	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	573	10	2	2	8.6	CC1CC(CC2CCC(N(C/C(Cl)=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)C(C)C2)CCC1N	10.1016/j.bmc.2007.06.003
		71458055	79028	0	None	-15	4	Human	5.1	pKi	=	5.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.7	CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		CHEMBL2113133	79028	0	None	-15	4	Human	5.1	pKi	=	5.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	6	2	5	3.7	CC(=O)N1CCCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		44434637	89412	0	None	-9	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.3	NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237052	89412	0	None	-9	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	377	11	2	2	4.3	NCCCCCN(CCCc1ccccc1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		71454495	78965	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113023	78965	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	614	8	3	6	3.2	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CN2CCCNCC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.10.096
		CHEMBL3667949	212143	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@@H]2CCCN2C1=O	nan
		44433406	167342	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)C4CCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL429445	167342	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	536	6	1	4	5.0	Cc1ccc(N2CCN(C(=O)[C@@H]3CN(C(=O)C4CCC4)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		44432958	87209	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		CHEMBL232775	87209	1	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	499	15	1	6	5.5	COCCNc1nc2ccc(C(=O)N(CCC(C)C)CCC(C)C)cc2n1CCCN1CCCCC1	10.1016/j.bmcl.2007.06.010
		44447812	95364	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256746	95364	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	496	5	1	4	4.4	CC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44415706	81147	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	599	10	1	4	7.1	CCC(C)[C@H](NCC1CCCO1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215741	81147	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	599	10	1	4	7.1	CCC(C)[C@H](NCC1CCCO1)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44456460	97475	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)cc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL270202	97475	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	601	10	1	5	4.6	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2cc(F)cc(F)c2)CC1	10.1016/j.bmcl.2007.10.115
		44434785	148791	0	None	-3	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	623	11	2	4	7.8	COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		CHEMBL394074	148791	0	None	-3	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	623	11	2	4	7.8	COc1cc(Br)c(CN(C(=O)CCCc2c[nH]c3ccccc23)[C@H]2CC[C@@H](C[C@H]3CC[C@@H](N)CC3)CC2)cc1OC	10.1016/j.bmc.2007.06.003
		44434561	89588	0	None	-1	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	433	13	1	2	6.6	CCCCCN(Cc1ccc(N(CC)CC)cc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237478	89588	0	None	-1	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	433	13	1	2	6.6	CCCCCN(Cc1ccc(N(CC)CC)cc1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44405361	135037	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		CHEMBL371945	135037	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	629	11	3	5	4.3	NC(C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1)c1ccccc1	10.1016/j.bmcl.2005.08.061
		44447817	95510	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL257373	95510	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	5	1	4	5.4	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)C(C)(C)C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		46885480	7754	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		CHEMBL1089103	7754	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	491	4	1	4	4.6	C[C@H]1CN(C(=O)[C@H]2CN(c3ccccn3)C[C@@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1ccccc1	10.1021/jm9017866
		44447239	153806	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.2	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL398236	153806	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	459	5	1	4	4.2	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2COCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL3644318	211958	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646853	211997	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](Cc3ccccc3Cl)CN2C1=O	nan
		CHEMBL3646863	212006	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644346	211985	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646890	212028	0	None	37	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		134149606	148538	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3Cl)CN2C1=O	nan
		CHEMBL3938651	148538	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL	1151	18	15	11	3.9	CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H]1C/C(O)=N\CCCC[C@H](C(N)=O)/N=C(/O)[C@@H](Cc2c[nH]c3ccccc23)/N=C(/O)[C@@H](CCCNC(=N)N)/N=C(/O)[C@H](Cc2ccccc2)/N=C(/O)[C@H]2C[C@H](Cc3ccccc3Cl)CN2C1=O	nan
		CHEMBL3644318	211958	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644346	211985	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCS(C)(=O)=O)NC1=O	nan
		CHEMBL3646863	212006	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCCN)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646890	212028	0	None	37	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		88287941	128652	0	None	23	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3667924	128652	0	None	23	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL	1080	18	17	12	-3.8	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2cc(F)cc(F)c2)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		CHEMBL3639667	211919	0	None	64	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccc(F)c(F)c2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3663347	212077	0	None	38	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CO)NC1=O	nan
		CHEMBL3663365	212094	0	None	-1	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3667959	212153	0	None	11	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2C(F)(F)F)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		25128749	178470	0	None	25	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
		CHEMBL466380	178470	0	None	25	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	560	10	2	4	3.2	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(C)=O	10.1021/jm800525p
		44412612	138925	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		CHEMBL378408	138925	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to human MC4R transfected in HEK293 cells	ChEMBL	621	11	2	5	4.8	CCN(CC(C1CCCCC1)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CC2Cc3ccccc3N2)CC1)C(C)=O	10.1016/j.bmcl.2006.04.002
		25058412	189440	0	None	120	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL513404	189440	0	None	120	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2008.07.076
		44416299	80558	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	471	8	1	4	5.2	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL214886	80558	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	471	8	1	4	5.2	COc1cc(Cl)ccc1C[C@@H](C)C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		168275776	190309	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5176092	190309	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5087839	215120	0	None	-11	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](C)C(=O)N2	10.1021/acs.jmedchem.1c00095
		16172929	213001	15	None	-9	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0501432
		CHEMBL412536	213001	15	None	-9	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cellsInhibition of [125I]NDP-alpha-MSH binding to melanocortin-4 receptor expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm0501432
		44562440	179041	0	None	27	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL471340	179041	0	None	27	3	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	534	10	3	5	3.7	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44432945	86796	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232186	86796	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44443034	154701	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	8	1	6	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc5c(c4)OCO5)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL399766	154701	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	580	8	1	6	5.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc5c(c4)OCO5)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		44432945	86796	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232186	86796	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	535	13	1	5	7.3	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(F)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44397030	67369	0	None	57	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	607	11	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL188651	67369	0	None	57	4	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	607	11	3	6	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3cccs3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		1338	3807	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		44433439	89924	0	None	44	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		CHEMBL237976	89924	0	None	44	3	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	538	6	1	5	4.8	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C4CCOCC4)C[C@@H]3c3ccc(Cl)cc3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2007.09.079
		16132144	209279	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44433268	152231	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	642	11	2	5	5.6	CC(C)C[C@H](NCCO)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL396884	152231	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	642	11	2	5	5.6	CC(C)C[C@H](NCCO)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24180493	155124	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL402043	155124	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	635	10	2	5	5.7	CC(C)C[C@H](NC(=O)CCN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44432946	86995	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232386	86995	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44434575	89309	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236872	89309	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44412898	77655	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	549	12	3	6	2.8	COCC(C)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL208860	77655	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	549	12	3	6	2.8	COCC(C)NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44416183	79844	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	475	7	1	3	5.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL212180	79844	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	475	7	1	3	5.9	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3Cl)CC2)c([C@@H](N)CC(C)C)c1	10.1016/j.bmcl.2006.06.075
		44432946	86995	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232386	86995	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	551	13	1	5	7.8	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(Cl)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		44397198	66765	0	None	93	3	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		CHEMBL185862	66765	0	None	93	3	Human	8.1	pKi	=	8.1	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	601	11	3	5	3.6	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(C2(CNC(=O)Cc3ccccc3)CCCCC2)CC1	10.1016/j.bmcl.2005.05.017
		44444502	154916	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL400933	154916	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	621	9	2	5	5.3	CC(C)C[C@H](NC(=O)CN)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		10414731	76548	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
		CHEMBL206141	76548	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	532	10	3	3	4.7	COc1ccc(Br)cc1CCc1c(F)cccc1C(=O)/N=C(\N)NCCCNC1CCCCC1	10.1016/j.bmcl.2006.01.016
		1338	3807	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		9938402	3807	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL339053	3807	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm0311285
		CHEMBL3644314	211954	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CN)NC1=O	nan
		CHEMBL3644314	211954	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CN)NC1=O	nan
		44405376	72003	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	620	11	2	5	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3cccs3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197435	72003	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	620	11	2	5	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)Cc3cccs3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44416184	79998	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	427	7	1	3	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL212779	79998	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	427	7	1	3	4.9	CC(C)C[C@H](N)c1ccccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		71458059	79050	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113155	79050	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	599	7	2	5	3.9	CN(C)[C@@H]1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44434754	90236	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238345	90236	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	557	11	3	4	7.2	COc1cc(O)ccc1/C=C/CN(C(=O)CCCc1c[nH]c2ccccc12)C1CCC(CC2CCC(N)CC2)CC1	10.1016/j.bmc.2007.06.003
		44401392	68657	0	None	-1	2	Human	5.1	pKi	=	5.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	582	14	5	4	3.1	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL191975	68657	0	None	-1	2	Human	5.1	pKi	=	5.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	582	14	5	4	3.1	N=C(N)NCCC[C@H](NC(=O)CCc1ccccc1)C(=O)N1C[C@H](Cc2ccccc2)C[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmcl.2005.03.120
		CHEMBL2221249	209443	0	None	-4	3	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	ChEMBL		None	None	None		CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@@H](CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O)[C@@H](C)O	nan
		44394081	66226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL184526	66226	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	653	11	3	5	4.9	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNCCc2ccc(F)cc2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44433478	167511	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	472	5	1	4	4.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL429985	167511	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	472	5	1	4	4.1	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		1338	3807	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		9938402	3807	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		CHEMBL339053	3807	43	None	53	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm050780s
		168281389	190922	0	None	-22	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5185405	190922	0	None	-22	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2149	33	33	26	-5.2	CCCC[C@@H]1NC(=O)[C@@H]2CSC3=C(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c4ccccc14)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2)C(=O)NC3=O	10.1021/acs.jmedchem.2c00793
		168284733	191624	0	None	-24	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5195641	191624	0	None	-24	3	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	2054	33	32	24	-4.1	CCCC[C@@H]1NC(=O)[C@@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		44447207	94541	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL251784	94541	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44447207	94541	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL251784	94541	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4 receptorBinding affinity to MC4 receptor	ChEMBL	509	7	1	3	6.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)(C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL2415018	210429	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL		None	None	None		CC(C)C(O)CCC(C)C(O)CCC(C)C(CCC(O)C(C)CCC(O)C(C)CCC(OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1)C(C)C)OCCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44434650	89899	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	11	2	2	4.8	NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL237910	89899	0	None	-2	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	11	2	2	4.8	NCCCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434600	148602	0	None	-7	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	9	2	2	4.0	NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393918	148602	0	None	-7	4	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	361	9	2	2	4.0	NCCCN(C/C=C/c1ccccc1)C(=O)CCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44413842	138377	0	None	-5	3	Human	5.1	pKi	=	5.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL377210	138377	0	None	-5	3	Human	5.1	pKi	=	5.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	587	14	5	6	1.3	NC(=O)C[C@H](N)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@@H](OCc2ccc3ccccc3c2)C[C@H]1CCCN=C(N)N	10.1021/jm060384p
		168279040	191182	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	481	3	1	5	5.3	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(Cl)cc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		CHEMBL5189093	191182	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting methodDisplacement of [125I]-[Nle4-D-phe7]-alpha-MSH from to human MC4R expressed in CHO cells incubated for 2 hrs by liquid scintillation counting method	ChEMBL	481	3	1	5	5.3	Cc1nc2c(cc1-c1ncccn1)CC[C@@]1(CCN(C(=O)C(C)c3ccc(Cl)cc3Cl)C1)N2	10.1021/acsmedchemlett.2c00229
		44433378	90188	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CNC[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL238208	90188	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.1	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CNC[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44405425	71860	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		CHEMBL197020	71860	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	669	10	3	5	4.5	NC1(C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N2CCN(C3(CNC(=O)Cc4ccccc4)CCCCC3)CC2)CCc2ccccc2C1	10.1016/j.bmcl.2005.08.061
		44415902	140028	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL380018	140028	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	509	8	1	4	5.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCC(=O)c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.06.075
		44562392	170356	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	645	12	1	6	6.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL444749	170356	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	645	12	1	6	6.8	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N(Cc2ccccn2)Cc2ccccn2)CC1	10.1016/j.bmcl.2008.07.076
		44577054	187616	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	431	6	1	3	4.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL494818	187616	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	431	6	1	3	4.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1	10.1016/j.bmc.2008.03.072
		CHEMBL438596	213781	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44434781	89904	0	None	-6	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL237919	89904	0	None	-6	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	485	9	2	2	7.0	NC1CCC(CC2CCC(N(Cc3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		137660993	159447	0	None	-213	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		CHEMBL4101216	159447	0	None	-213	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay	ChEMBL	1680	20	21	21	-3.5	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.8b00170
		44393820	66678	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		CHEMBL185427	66678	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	635	10	2	5	5.1	CN(Cc1ccccc1)Cc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.06.059
		44405402	71963	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	2	4	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccccc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL197329	71963	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	600	10	2	4	4.9	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccccc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		11249545	66204	0	None	-141	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1	10.1021/jm0400496
		CHEMBL184432	66204	0	None	-141	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	529	6	3	3	5.6	C[C@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)[C@H](C)CN1	10.1021/jm0400496
		11375764	66689	0	None	-398	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		CHEMBL185469	66689	0	None	-398	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity for human melanocortin 4 receptorBinding affinity for human melanocortin 4 receptor	ChEMBL	515	6	3	3	5.2	C[C@@H]1CN(/C(=N/c2ccc(C(=O)NCCc3ccc(Cl)cc3Cl)cc2)NC2CCCCC2)CCN1	10.1021/jm0400496
		44444447	94062	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	0	5	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCN(C)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL248963	94062	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	0	5	3.9	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCN(C)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44434861	90247	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238367	90247	0	None	-1	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	389	7	2	2	4.8	N[C@H]1CC[C@H](N(Cc2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		44434649	145812	0	None	-3	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	12	2	2	6.4	NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL391705	145812	0	None	-3	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	453	12	2	2	6.4	NCCCCCN(/C=C/Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		46885816	7906	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		CHEMBL1090161	7906	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	436	4	1	3	4.4	CCC[C@]1(O)[C@@H](C)CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@H]1C	10.1021/jm9017866
		44456416	167242	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	555	10	1	6	4.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccoc2)CC1	10.1016/j.bmcl.2007.10.115
		CHEMBL429252	167242	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	555	10	1	6	4.0	CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccoc2)CC1	10.1016/j.bmcl.2007.10.115
		44432918	152516	1	None	-	1	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	591	14	2	7	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCNC(=O)OC(C)(C)C)cc1	10.1016/j.bmcl.2007.06.010
		CHEMBL397140	152516	1	None	-	1	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	591	14	2	7	7.4	CC(=O)c1ccc(Nc2nc3ccc(C(=O)N(CCC(C)C)CCC(C)C)cc3n2CCCNC(=O)OC(C)(C)C)cc1	10.1016/j.bmcl.2007.06.010
		44396120	66936	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	540	9	2	6	2.4	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(C)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL186629	66936	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligandBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells was determined by using [125I]NDP-MSH as radioligand	ChEMBL	540	9	2	6	2.4	CC(c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCN)CC1)N1CCN(C)CC1	10.1016/j.bmcl.2004.08.055
		CHEMBL3644327	211967	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		CHEMBL3644327	211967	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		N=C(N)NCCC[C@H](N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC1=O	nan
		44415346	81315	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL215886	81315	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	481	7	1	3	5.7	CCC(C)[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2006.05.088
		44392514	123867	0	None	2	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		CHEMBL362670	123867	0	None	2	4	Human	6.1	pKi	=	6.1	Binding	Binding affinity towards Melanocortin 4 receptor using [125I]NDP-MSHBinding affinity towards Melanocortin 4 receptor using [125I]NDP-MSH	ChEMBL	575	7	2	7	3.0	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN([C@H]2CCCC[C@@H]2n2cncn2)CC1)C1Cc2ccccc2CN1	10.1021/jm0311285
		88944347	143186	0	None	-13182	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3896173	143186	0	None	-13182	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1067	19	15	12	-2.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CNC(=O)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44323234	168056	0	None	-7	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		CHEMBL432377	168056	0	None	-7	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity for human Melanocortin-4 receptor (hMC4R)Binding affinity for human Melanocortin-4 receptor (hMC4R)	ChEMBL	903	11	12	9	0.3	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)CCC(=O)NCCCC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm020021z
		44322812	112382	0	None	-2	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL329586	112382	0	None	-2	3	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	711	19	10	7	0.0	N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		44391316	123940	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	658	11	3	7	3.4	CC(NCCN1CCOCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL362841	123940	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	658	11	3	7	3.4	CC(NCCN1CCOCC1)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL3644279	211923	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644279	211923	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		44444511	94009	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		CHEMBL248687	94009	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	642	9	1	5	5.8	CC(C)C[C@H](NS(C)(=O)=O)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(C)C)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.06.088
		44447235	94949	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		CHEMBL254487	94949	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	588	10	1	5	5.6	CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@@H]2CCO[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.11.128
		44412896	139463	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	3	7	2.2	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		CHEMBL379417	139463	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	550	12	3	7	2.2	COCC(C)NCc1cccnc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CCN)CC1	10.1016/j.bmcl.2006.04.069
		44562496	186732	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	478	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CO)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL488716	186732	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	478	8	3	5	2.2	NCCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CO)CC1	10.1016/j.bmcl.2008.07.076
		9842665	156806	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		44434664	88558	0	None	-2	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL235355	88558	0	None	-2	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	378	10	3	3	3.2	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL3644280	211924	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644280	211924	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3644359	211993	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)NC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		CHEMBL3644359	211993	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)NC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC1=O	nan
		44265473	206356	1	None	9	2	Human	5.1	pKi	=	5.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	200	4	2	2	1.9	NCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL8743	206356	1	None	9	2	Human	5.1	pKi	=	5.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	200	4	2	2	1.9	NCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		10050686	76016	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		CHEMBL205553	76016	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	476	11	2	3	5.3	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1CCc1cccc2ccccc12	10.1016/j.bmcl.2006.01.016
		44562364	176986	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	10	2	5	5.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL462559	176986	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	547	10	2	5	5.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NCC2CCOC2)CC1	10.1016/j.bmcl.2008.07.076
		71450911	78961	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	N[C@H]1CCCC[C@@H]1NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		CHEMBL2113019	78961	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Binding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSHBinding affinity towards human melanocortin 4 receptor expressed in HEK 293 cells using [125I]NDP-MSH	ChEMBL	628	9	4	6	3.8	N[C@H]1CCCC[C@@H]1NCc1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H]2Cc3ccccc3CN2)CC1	10.1016/j.bmcl.2004.10.096
		44415659	78049	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	2	4	6.3	CCC(C)[C@H](NC[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL209954	78049	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	572	10	2	4	6.3	CCC(C)[C@H](NC[C@H](C)N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		168279267	191000	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186603	191000	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		88944179	151052	0	None	-1380	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	16	13	10	-1.3	CCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3958741	151052	0	None	-1380	2	Human	6.1	pKi	=	6.1	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	924	16	13	10	-1.3	CCCC(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		9842665	156806	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		CHEMBL40711	156806	12	None	-3	2	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL	376	5	1	3	3.7	COc1ccc(Br)cc1CCc1c(F)cccc1C1=NCCN1	10.1021/jm050780s
		11851038	140335	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		CHEMBL380691	140335	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL	497	6	0	5	5.2	CN(C)[C@H]1C[C@@H](C(=O)N2CCC(Cn3cncn3)(C3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1021/jm050780s
		24740310	89253	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		CHEMBL236804	89253	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	448	7	1	4	4.7	CC(C)C[C@H](N)c1cccnc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1021/jm701137s
		44265351	205765	0	None	-1	3	Human	4.1	pKi	=	4.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	8	2	3	4.7	N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		CHEMBL8287	205765	0	None	-1	3	Human	4.1	pKi	=	4.1	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	426	8	2	3	4.7	N[C@H](CCC(=O)O)C(=O)N(Cc1ccc2ccccc2c1)Cc1cccc2ccccc12	10.1016/s0960-894x(02)00088-4
		168277543	190675	0	None	-8	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		CHEMBL5181752	190675	0	None	-8	3	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	1347	15	14	15	1.3	CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](NC(C)=O)CCSCc2ccc(cc2)CSCC[C@H](C(N)=O)NC1=O	10.1021/acs.jmedchem.2c00793
		44562561	174254	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454906	174254	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	520	9	3	5	3.4	CC(C)C[C@@H](O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL3644350	211989	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3646865	212008	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		88227239	153420	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	18	17	12	-3.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3979009	153420	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	18	17	12	-3.6	CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3644338	211978	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644357	211991	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Assay Using [I125]-NDP-a-MSH: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37° C., the assay mixture was filtered and the membranes washed three times with ice-cold buffer. Filters were dried and counted in a gamma counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Radioactivity (cpm) obtained in the presence of test compounds was normalized with respect to 100% specific binding to determine the percent inhibition of [I125]-NDP-α-MSH binding. Each assay was conducted in triplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for test peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC[S+](C)[O-])NC1=O	nan
		CHEMBL3644338	211978	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644350	211989	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCN)NC1=O	nan
		CHEMBL3644357	211991	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC[S+](C)[O-])NC1=O	nan
		CHEMBL3646865	212008	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3646871	212010	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3663377	212106	0	None	3	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@H](CN)NC1=O	nan
		CHEMBL3667918	212115	0	None	38	2	Human	8.1	pKi	=	8.1	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.Competitive Inhibition Assay: A competitive inhibition binding assay was performed for exemplified peptides according to the invention using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 60 minutes at 37 C., the assay mixture was filtered and the membranes washed.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CCCNC(=O)CC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2F)NC(=O)[C@H](CC(N)=O)NC1=O	nan
		168275776	190309	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5176092	190309	0	None	-	1	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	100	37	39	-8.1	CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(N)=O	10.1021/acs.jmedchem.2c00786
		1324	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16154396	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		16197727	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		44285019	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		57514683	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		91898441	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		CHEMBL441738	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		DB04931	302	25	None	-3	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	ChEMBL		None	None	None		None	10.1021/jm050780s
		25129107	173777	0	None	19	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
		CHEMBL453734	173777	0	None	19	3	Human	8.1	pKi	=	8.1	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	603	11	3	5	2.9	CCC[C@H]1C(=O)N([C@@H](Cc2ccc3ccccc3c2)C(=O)NC)CCN1C(=O)[C@@H](Cc1ccc(F)cc1)NC(=O)C(C)(C)N	10.1021/jm800525p
		1338	3807	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.03.120
		9938402	3807	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.03.120
		CHEMBL339053	3807	43	None	53	4	Human	8.1	pKi	=	8.1	Binding	Inhibitory activity towards human Melanocortin 4 ReceptorInhibitory activity towards human Melanocortin 4 Receptor	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1016/j.bmcl.2005.03.120
		23661656	169044	0	None	-1	5	Rat	8.0	pKi	=	8.0	Binding	Binding affinity to rat MC4 receptorBinding affinity to rat MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL439560	169044	0	None	-1	5	Rat	8.0	pKi	=	8.0	Binding	Binding affinity to rat MC4 receptorBinding affinity to rat MC4 receptor	ChEMBL	564	8	1	4	5.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		44416327	80601	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.6	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215066	80601	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	491	8	1	4	5.6	COc1cc(Cl)ccc1CC(C)C(=O)N1CCN(c2ccc(Cl)cc2[C@@H](N)CC(C)C)CC1	10.1016/j.bmcl.2006.06.075
		44433481	148890	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	4	5.8	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL394161	148890	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	540	6	1	4	5.8	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H]2CN(C3CCCCC3)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		16132144	209279	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		16133793	209279	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44273719	209279	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		CHEMBL214332	209279	36	None	-30	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	10.1021/jm050780s
		44562287	174248	0	None	102	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454900	174248	0	None	102	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	3.9	CCC(O)(CC)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL409636	212773	0	None	-1	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.Binding affinity against Melanocortin 4 receptor by gamma-MCH displacement.	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(C)C)C(=O)N[C@H]1CC(=O)NCCCC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC1=O	10.1021/jm030119t
		25211670	174260	0	None	56	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL454916	174260	0	None	56	3	Human	8.0	pKi	=	8.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	548	10	2	5	4.0	CC(C)CC(O)c1ccccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)NC(=O)CN(C)C)CC1	10.1016/j.bmcl.2008.07.076
		24741625	89192	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		CHEMBL236731	89192	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Binding affinity at human MC4RBinding affinity at human MC4R	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmcl.2007.07.097
		24741625	89192	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		CHEMBL236731	89192	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from MC4R receptor in HEK293 cellsDisplacement of [125I]NDP-MSH from MC4R receptor in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1016/j.bmc.2007.05.026
		23634986	91438	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		23634986	91438	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		CHEMBL240357	91438	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmc.2008.03.072
		CHEMBL240357	91438	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	441	6	1	3	5.1	Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3C)CC2)c([C@@H](N)C(C)C)c1	10.1021/jm070806a
		44432951	86792	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232163	86792	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		24741625	89192	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		CHEMBL236731	89192	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	548	8	1	4	5.1	CC(C)C[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1	10.1021/jm701137s
		44432951	86792	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		CHEMBL232163	86792	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cellsDisplacement of [125I]NDP-alphaMSH from human melanocortin 4 receptor expressed in CHOK1 cells	ChEMBL	600	14	1	6	8.2	CC(C)CCN(CCC(C)C)C(=O)c1ccc2nc(Nc3ccc(N4CCCCC4)cc3)n(CCCN3CCCCC3)c2c1	10.1016/j.bmcl.2007.06.010
		1338	3807	43	None	53	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		9938402	3807	43	None	53	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		CHEMBL339053	3807	43	None	53	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	588	8	2	6	4.6	O=C([C@@H]1NCc2c(C1)cccc2)N[C@@H](C(=O)N1CCC(CC1)(Cn1cncn1)C1CCCCC1)Cc1ccc(cc1)Cl	10.1021/jm049278i
		44394009	124350	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		CHEMBL363684	124350	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptorDisplacement of [125I]NDP-MSH from HEK293 cells expressing human melanocortin-4 receptor	ChEMBL	571	9	3	5	3.7	O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)N1CCN(c2ccccc2CNC2CC2)CC1)[C@H]1Cc2ccccc2CN1	10.1016/j.bmcl.2004.06.059
		44456368	95524	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL257447	95524	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	595	10	1	5	5.2	Cc1ccc(N2CCN(C(=O)[C@H]3CN(C(C)C)C[C@H]3c3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1	10.1016/j.bmcl.2007.10.115
		CHEMBL438596	213781	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	ChEMBL		None	None	None		CC[C@@H](C)[C@H]1NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C1=O	10.1021/jm050780s
		44443022	154799	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		CHEMBL400249	154799	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [12]NDPMSH from human MC4R expressed in HEK293 cellsDisplacement of [12]NDPMSH from human MC4R expressed in HEK293 cells	ChEMBL	570	8	1	4	6.1	CC(C)N1C[C@H](c2ccc(Cl)cc2)[C@@H](C(=O)N2CCN(C3(CNCc4ccc(Cl)cc4)CCCCC3)CC2)C1	10.1016/j.bmcl.2007.10.032
		11846673	79994	0	None	3	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		CHEMBL212766	79994	0	None	3	3	Human	7.1	pKi	=	7.1	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	515	11	3	4	3.1	CC(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](OCc2ccc3ccccc3c2)C[C@@H]1CCCN=C(N)N	10.1021/jm060384p
		44404560	172552	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		CHEMBL448473	172552	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Inhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptorInhibition of [125I]-NDP MSH binding to human Melanocortin 4 receptor	ChEMBL	275	6	0	3	2.3	CCN(CC)CC(c1ccccc1)N1CCN(C)CC1	10.1016/j.bmcl.2005.08.018
		10075878	75991	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL205461	75991	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	536	12	2	5	4.7	CCN(CC)CCCC(C)/N=C(/N)NC(=O)c1cccc(F)c1OCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		70685980	75073	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	337	6	3	3	1.5	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		CHEMBL2035935	75073	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation countingDisplacement of [125I]NDPMSH from human MC4 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counting	ChEMBL	337	6	3	3	1.5	O=C(NCc1ccccc1)[C@@H]1CNC[C@H]1C(=O)NCc1ccccc1	10.1016/j.bmc.2012.04.001
		44404822	70298	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	3.1	CS(=O)(=O)N1CCCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		CHEMBL194368	70298	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	635	7	2	6	3.1	CS(=O)(=O)N1CCCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		44404823	125399	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	621	7	2	6	2.8	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		CHEMBL364553	125399	0	None	-	1	Human	6.1	pKi	=	6.1	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	621	7	2	6	2.8	CS(=O)(=O)N1CCc2cccc(N3CCN(C(=O)C(Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c21	10.1016/j.bmcl.2005.07.035
		44562438	178935	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	560	10	2	5	4.6	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL470301	178935	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human MC4 receptorBinding affinity to human MC4 receptor	ChEMBL	560	10	2	5	4.6	CNC(C)(C)C(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(=O)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		168279267	191000	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		CHEMBL5186603	191000	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	3071	96	36	39	-7.5	CC(C)C[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)N1C(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)Cc2ccccc21)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)O	10.1021/acs.jmedchem.2c00786
		168294114	192190	0	None	-40	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4756	82	66	59	-5.7	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5204285	192190	0	None	-40	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL	4756	82	66	59	-5.7	CCCC[C@@H]1NC(=O)[C@@H]2CSc3nnc(c4c3CCC3C(CC4)C3COC(=O)NCCOCCOCCOCCNC(=O)OCC3C4CCc5c6nnc(c5CCC43)SC[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](CS6)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](Cc4cnc[nH]4)NC3=O)SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)CNC1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.2c00793
		CHEMBL5078687	214580	0	None	-6	3	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assayDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay	ChEMBL		None	None	None		CC[C@H](C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)N(C)C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]2CSSC[C@H](NC1=O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c3ccccc13)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2	10.1021/acs.jmedchem.1c00095
		44415767	80285	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		CHEMBL214000	80285	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	543	9	1	3	7.0	CCN[C@H](c1cc(C(F)(F)F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1)C(C)CC	10.1016/j.bmcl.2006.05.088
		44444448	94063	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL248964	94063	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	523	6	1	5	4.0	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCC(N)CC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		44416251	141881	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		CHEMBL386707	141881	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	489	7	1	3	5.9	Cc1ccc(CC(C)C(=O)N2CCN(c3ccc(C(F)(F)F)cc3[C@@H](N)CC(C)C)CC2)c(C)c1	10.1016/j.bmcl.2006.06.075
		44447818	95410	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		CHEMBL256956	95410	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	613	6	2	5	5.1	Cc1ccc(N2CCN(C(=O)[C@@H]3[C@@H](c4ccc(Cl)cc4)CCN3C(=O)[C@H]3Cc4ccccc4CN3)CC2)c([C@@H](N)C(C)C)c1	10.1016/j.bmcl.2008.01.125
		44397122	66855	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	598	11	3	6	3.9	N#Cc1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		CHEMBL186227	66855	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells Inhibition of [125I]NDP-MSH (radioligand) binding to the hMC4R stably expressed in HEK293 cells	ChEMBL	598	11	3	6	3.9	N#Cc1ccc(CNCC2(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4Cl)NC(=O)CCN)CC3)CCCCC2)cc1	10.1016/j.bmcl.2005.05.017
		10072440	76015	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	8	2	3	4.2	CCCC/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		CHEMBL205552	76015	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Binding affinity to MC4R by membrane filtration assayBinding affinity to MC4R by membrane filtration assay	ChEMBL	449	8	2	3	4.2	CCCC/N=C(/N)NC(=O)c1cccc(F)c1CCc1cc(Br)ccc1OC	10.1016/j.bmcl.2006.01.016
		44415985	81084	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		CHEMBL215519	81084	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R stably expressed in HEK293 cells	ChEMBL	495	7	1	3	5.9	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C(C)Cc2cccc(Cl)c2)CC1	10.1016/j.bmcl.2006.06.075
		44434782	90027	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	511	10	2	2	7.5	NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL238144	90027	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	511	10	2	2	7.5	NC1CCC(CC2CCC(N(C/C=C/c3ccccc3)C(=O)CCCc3c[nH]c4ccccc34)CC2)CC1	10.1016/j.bmc.2007.06.003
		44434856	154392	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	535	14	2	4	5.0	NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		CHEMBL398777	154392	0	None	-1	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	535	14	2	4	5.0	NCCCN1CCN(CCCN(C/C(Cl)=C/c2ccccc2)C(=O)CCCc2c[nH]c3ccccc23)CC1	10.1016/j.bmc.2007.06.003
		88944401	146250	0	None	-9332	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	16	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		CHEMBL3920516	146250	0	None	-9332	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	965	16	13	10	-0.5	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)CC2CCCC2)CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O	nan
		168282596	190906	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2990	66	33	37	-3.8	CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.2c00786
		CHEMBL5185132	190906	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysisDisplacement of [125I]-NDP-alpha-MSH from human MC4R expressed in CHO cells by Topcount beta counter analysis	ChEMBL	2990	66	33	37	-3.8	CC(C)C[C@@H]1NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CC(C)C)CSSC[C@@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCN2C(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O	10.1021/acs.jmedchem.2c00786
		44348046	16512	0	None	-	1	Human	5.0	pKi	=	5.0	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	4	1	3	5.0	Cn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1O	10.1016/j.bmcl.2004.05.003
		CHEMBL123660	16512	0	None	-	1	Human	5.0	pKi	=	5.0	Binding	In vitro binding affinity towards melanocortin 4 receptor.In vitro binding affinity towards melanocortin 4 receptor.	ChEMBL	390	4	1	3	5.0	Cn1ccnc1-c1cccc(Cl)c1CCc1cc(Br)ccc1O	10.1016/j.bmcl.2004.05.003
		44400834	127394	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	516	9	2	5	4.6	N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		CHEMBL365940	127394	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Binding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligandBinding affinity for melanocortin-4 receptor transfected in HEK 293 cells using [125I]NDP-MSH as radioligand	ChEMBL	516	9	2	5	4.6	N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2CNCCc2cccs2)CC1	10.1016/j.bmcl.2005.03.053
		44433482	169446	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2CN(Cc3ccccc3)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL442703	169446	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)C2CN(Cc3ccccc3)CC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44415418	80147	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		CHEMBL213381	80147	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	465	7	1	3	5.5	CC(C)C[C@H](N)c1cc(F)ccc1N1CCN(C(=O)CCc2ccc(Cl)cc2Cl)CC1	10.1016/j.bmcl.2006.05.088
		44447801	168777	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	5	4.7	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL437406	168777	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	512	6	1	5	4.7	CCOC(=O)N1CC[C@H](c2ccc(Cl)cc2)[C@@H]1C(=O)N1CCN(c2ccccc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		44434648	148159	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.1	NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL393558	148159	0	None	-2	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	413	10	2	2	5.1	NCCCCCN(CCc1ccc2ccccc2c1)C(=O)Cc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44265309	205662	1	None	-2	3	Human	4.0	pKi	=	4.0	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	214	5	2	2	2.3	NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL8201	205662	1	None	-2	3	Human	4.0	pKi	=	4.0	Binding	Tested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assayTested for its binding affinity towards human recombinant Melanocortin 4 receptor by using radioligand binding assay	ChEMBL	214	5	2	2	2.3	NCCCNCc1ccc2ccccc2c1	10.1016/s0960-894x(02)00088-4
		CHEMBL3644304	211947	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.Competitive Binding Assay Using Eu-NDP-a-MSH: A competitive inhibition binding assay was performed employing Eu-NDP-α-MSH (PerkinElmer Life Sciences catalog No. AD0225) with determination by time-resolved fluorometry (TRF) of the lanthanide chelate. In comparison studies with [I125]-NDP-α-MSH, the same values, within experimental error ranges, were obtained for percent inhibition and Ki. Typically competition experiments to determine Ki values were conducted by incubating membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R with 9 different concentrations of test compounds of interest and 2 nM of Eu-NDP-α-MSH in a solution containing 25 mM HEPES buffer with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2 and 0.3 mM 1,10-phenanthroline. After incubation for 90 minutes at 37° C., the reaction was stopped by filtration over AcroWell 96-well filter plates (Pall Life Sciences). The filter plates were washed 4 times with 200 uL of ice-cold phosphate-buffered saline. DELFIA Enhancement solution (PerkinElmer Life Sciences) was added to each well. The plates were incubated on a shaker for 15 minutes and read at 340 nm excitation and 615 nm emission wavelengths. Each assay was conducted in duplicate and mean values were utilized. Ki values were determined by curve-fitting with Graph-Pad Prism software using a one-site fixed-slope competition binding model.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	nan
		CHEMBL3644304	211947	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.Competitive Inhibition Assay: A competitive inhibition binding assay is performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMC4-R, hMC3-R, or hMC5-R, and from B-16 mouse melanoma cells (containing endogenous MC1-R). In some instances, HEK-293 cells that express recombinant hMC1-R were employed. In the examples that follow, all MC3-R, MC4-R and MC5-R values are for human recombinant receptors. MC1-R values are for B-16 mouse melanoma cells, unless the heading is hMC1-R, in which case the value is for human recombinant MC1-R. Assays were performed in 96 well GF/B Millipore multiscreen filtration plates (MAFB NOB10) pre-coated with 0.5% bovine serum albumin (Fraction V). Membrane homogenates were incubated with 0.2 nM (for hMC4-R) 0.4 nM (for MC3-R and MC5-R) or 0.1 nM (for mouse B16 MC1-R or hMC1-R) [I125]-NDP-alpha -MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl.	ChEMBL		None	None	None		CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]cn2)NC1=O	nan
		88944292	150598	0	None	-2398	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1001	21	14	11	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		CHEMBL3955172	150598	0	None	-2398	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1001	21	14	11	-1.3	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O	nan
		44433383	88530	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	7	1	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(S(C)(=O)=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL235214	88530	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	600	7	1	5	4.7	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(S(C)(=O)=O)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		10304463	76774	0	None	9	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	615	11	1	5	5.6	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.10.103
		CHEMBL206840	76774	0	None	9	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-alpha-MSH from cloned human MC4R expressed in HEK293 cells	ChEMBL	615	11	1	5	5.6	CCN(CC)CC(c1ccccc1F)N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)c2cc3ccccc3cn2)CC1	10.1016/j.bmcl.2005.10.103
		44444445	154846	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	0	4	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		CHEMBL400511	154846	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	508	6	0	4	5.1	CC(C)N1C[C@@H](C(=O)N2CCN(c3ccccc3CN3CCCCC3)CC2)[C@H](c2ccc(Cl)cc2)C1	10.1016/j.bmcl.2007.06.088
		71452731	79033	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.5	CC(C)S(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		CHEMBL2113138	79033	0	None	-	1	Human	6.0	pKi	=	6.0	Binding	Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptorInhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor	ChEMBL	663	8	2	6	3.5	CC(C)S(=O)(=O)N1CCc2cccc(N3CCN(C(=O)[C@@H](Cc4ccc(Cl)cc4)NC(=O)[C@H]4Cc5ccccc5CN4)CC3)c2C1	10.1016/j.bmcl.2005.07.035
		44433382	88488	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	2	5	4.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)CN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL234993	88488	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	579	7	2	5	4.3	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H]2CN(C(=O)CN)C[C@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44447768	95611	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	488	6	2	4	4.8	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL257827	95611	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	488	6	2	4	4.8	CC(C)C[C@H](N)c1cc(Cl)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		44347110	114109	0	None	5	3	Human	6.0	pKi	=	6.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	681	9	9	7	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		CHEMBL332762	114109	0	None	5	3	Human	6.0	pKi	=	6.0	Binding	Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)Binding affinity against human melanocortin receptor 4 (hMC4R) (concentration of the peptide at 50% specific binding)	ChEMBL	681	9	9	7	0.6	N=C(N)NCCC[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NCC(=O)CC[C@H](C(N)=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O	10.1021/jm010165y
		44434841	88701	0	None	-30	3	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	455	11	4	2	4.9	N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL236022	88701	0	None	-30	3	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	455	11	4	2	4.9	N=C(N)NCCCCN(Cc1ccc2ccccc2c1)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		44434659	147946	0	None	-2	2	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	384	11	2	5	2.6	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc([N+](=O)[O-])cc1	10.1016/j.bmc.2007.06.003
		CHEMBL393382	147946	0	None	-2	2	Human	4.0	pKi	=	4.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	384	11	2	5	2.6	NCCCCCN(Cc1ccccc1)C(=O)[C@H](N)Cc1ccc([N+](=O)[O-])cc1	10.1016/j.bmc.2007.06.003
		44405403	140351	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	618	10	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccc(F)cc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL380768	140351	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	618	10	2	4	5.0	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)c3ccc(F)cc3)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		44447808	95324	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	476	5	1	4	4.0	CC(=O)N1CC[C@H](c2ccc(C)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL256539	95324	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	476	5	1	4	4.0	CC(=O)N1CC[C@H](c2ccc(C)cc2)[C@@H]1C(=O)N1CCN(c2ccc(C)cc2[C@@H](N)C(C)C)CC1	10.1016/j.bmcl.2008.01.125
		46885759	8276	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
		CHEMBL1092548	8276	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	488	3	1	3	4.9	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1cccc(F)c1	10.1021/jm9017866
		44413828	139293	0	None	5	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		CHEMBL379168	139293	0	None	5	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	632	12	5	5	4.0	N=C(N)NCCC[C@H]1C[C@H](OCc2ccc3ccccc3c2)CN1C(=O)[C@@H](Cc1ccccc1)NC(=O)C1Cc2ccccc2CN1	10.1021/jm060384p
		44322986	106097	0	None	-2	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		CHEMBL313377	106097	0	None	-2	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity towards human melanocortin 4 receptor (hMC4R)Binding affinity towards human melanocortin 4 receptor (hMC4R)	ChEMBL	713	19	9	7	0.1	CC(C)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1016/s0960-894x(03)00552-3
		88878683	143852	0	None	-1949	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	973	19	14	11	-2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		CHEMBL3901634	143852	0	None	-1949	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	973	19	14	11	-2.0	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCN)NC1=O	nan
		88944297	154150	0	None	-218	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	21	15	11	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		CHEMBL3985463	154150	0	None	-218	2	Human	7.0	pKi	=	7.0	Binding	Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.Competitive Inhibition Binding Assay: A competitive inhibition binding assay was performed using membrane homogenates prepared from HEK-293 cells that express recombinant hMCR-1a or hMCR-4 (in each instance where the h prefix refers to human), or alternatively membrane homogenates from B16-F10 mouse melanoma cells containing endogenous murine MCR-1. In the examples that follow, all MCR-1 and MCR-4 values are for human recombinant receptors, unless otherwise noted. Assays were performed in 96 well polypropylene round-bottom plates (VWR catalog number 12777-030). Membrane homogenates were incubated with 0.1 nM [I125]-NDP-α-MSH (Perkin Elmer) and increasing concentrations of test peptides of the present invention in buffer containing 25 mM HEPES buffer (pH 7.5) with 100 mM NaCl, 2 mM CaCl2, 2 mM MgCl2, 0.3 mM 1,10-phenanthroline, and 0.2% bovine serum albumin. After incubation for 90 minutes at 37° C., the assay mixture was filtered onto GF/B Unifilter plates (Perkin-Elmer catalog number 6005177) and washed with 3 mL of ice-cold buffer per well. Filters were air dried and 35 uL of scintillation cocktail added to each well. Plates were counted in a Microbeta counter for bound radioactivity. Non-specific binding was measured by inhibition of binding of [I125]-NDP-α-MSH in the presence of 1 uM NDP-α-MSH. Maximal specific binding (100%) was defined as the difference in radioactivity (cpm) bound to cell membranes in the absence and presence of 1 uM NDP-α-MSH. Each assay was conducted in duplicate and the actual mean values are described, with results less than 0% reported as 0%. Ki values for peptides of the present invention were determined using Graph-Pad Prism curve-fitting software.	ChEMBL	1030	21	15	11	-1.9	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CCC(=O)NCC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(N)=O)NC1=O	nan
		44433484	89194	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CN(Cc3ccccc3)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		CHEMBL236737	89194	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	548	7	1	4	5.7	CC(C)[C@H](N)c1cccc(F)c1N1CCN(C(=O)[C@H]2CN(Cc3ccccc3)C[C@@H]2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2007.09.079
		44447767	155639	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		CHEMBL404710	155639	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cellsDisplacement of [125]NDPMSH from human MC4 receptor expressed in HEK293 cells	ChEMBL	522	6	2	4	5.2	CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)C2NCCC2c2ccc(Cl)cc2)CC1	10.1016/j.bmcl.2008.01.125
		25128748	189991	0	None	28	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
		CHEMBL517108	189991	0	None	28	3	Human	7.0	pKi	=	7.0	Binding	Displacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cellsDisplacement of europium-labeled NDP-alpha-MSH from human MC4R expressed in HEK293 cells	ChEMBL	490	7	2	4	2.3	CNC(=O)[C@H](Cc1ccc2ccccc2c1)N1CCN(C(=O)[C@H](N)Cc2ccc(F)cc2)[C@@H](C)C1=O	10.1021/jm800525p
		44434686	146600	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	407	11	3	3	4.7	CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		CHEMBL392316	146600	0	None	-3	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	407	11	3	3	4.7	CC(Cc1ccccc1)CN(CCCCCCN)C(=O)c1cc2cc(O)ccc2[nH]1	10.1016/j.bmc.2007.06.003
		44434595	148872	0	None	-1	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	419	9	2	3	5.6	CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL394149	148872	0	None	-1	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	419	9	2	3	5.6	CC(c1csc2ccccc12)N(CCCN)C(=O)CCCc1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL1923663	209086	0	None	-549	3	Human	6.0	pKi	=	6	Binding	Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysisDisplacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL		None	None	None		CC(=O)N[C@@H](CCc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O	10.1021/jm201226w
		44562476	186015	0	None	-	1	Human	7.0	pKi	=	7	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		CHEMBL487044	186015	0	None	-	1	Human	7.0	pKi	=	7	Binding	Binding affinity to human MC4 receptor Asp122Ala mutantBinding affinity to human MC4 receptor Asp122Ala mutant	ChEMBL	533	10	3	5	3.6	CNCC(=O)N[C@H](Cc1ccc(Cl)cc1Cl)C(=O)N1CCN(c2ccccc2C(N)CC(C)C)CC1	10.1016/j.bmcl.2008.07.076
		44405362	168283	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		CHEMBL433991	168283	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cellsDisplacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells	ChEMBL	641	10	3	5	4.4	O=C(Cc1ccccc1)NCC1(N2CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3NCc4ccccc43)CC2)CCCCC1	10.1016/j.bmcl.2005.08.061
		46885760	8278	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
		CHEMBL1092550	8278	0	None	-	1	Human	7.0	pKi	=	7	Binding	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	ChEMBL	506	3	1	3	5.1	C[C@H]1CN(C(=O)[C@@H]2CN(C(C)(C)C)C[C@H]2c2ccc(F)cc2F)C[C@@H](C)[C@]1(O)c1c(F)cccc1F	10.1021/jm9017866
		46930943	68405	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		CHEMBL1917059	68405	0	None	-	1	Human	6.0	pKi	=	6	Binding	Displacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assayDisplacement of Eu-DTPA-PEGO-NDP-alpha-MSH-NH2 from human MC4R expressed in HEL293 cells after 1 hr by time-resolved fluorescence assay	ChEMBL	864	27	10	10	1.8	CCCCc1cn(CCCCCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)nn1	10.1016/j.bmc.2013.06.052
		44265672	10181	0	None	-4	4	Human	5.0	pKi	=	5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	442	10	5	3	3.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00089-6
		CHEMBL1159699	10181	0	None	-4	4	Human	5.0	pKi	=	5	Binding	Binding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptorBinding affinity in competition with [125I]NDP-MSH on recombinant melanocortin 4 receptor	ChEMBL	442	10	5	3	3.1	NC(N)=NCCC[C@H](NCc1ccc2ccccc2c1)C(=O)NCc1c[nH]c2ccccc12	10.1016/s0960-894x(02)00089-6
		44434656	90023	0	None	-37	3	Human	4.0	pKi	=	4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	401	10	2	2	5.2	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		CHEMBL238136	90023	0	None	-37	3	Human	4.0	pKi	=	4	Binding	Displacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cellsDisplacement of [125I]NDP-MSH from human recombinant MC4 receptor expressed in Sf9 cells	ChEMBL	401	10	2	2	5.2	C/C(=C/c1ccccc1)CN(CCCCCN)C(=O)/C=C/c1c[nH]c2ccccc12	10.1016/j.bmc.2007.06.003
		10408	720	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		5329	720	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		9941379	720	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		CHEMBL2070241	720	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		DB11653	720	28	None	1	4	Human	8.1	pKd	=	8.1	Binding	Functional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4RFunctional evaluation of PT‐141 at the MC4R was performed by measuring the accumulation of intracellular cAMP in HEK‐293 cells expressing MC4R	Drug Central		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	None
		11993702	3593	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		5416	3593	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		9272	3593	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		CHEMBL3301624	3593	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		DB11700	3593	18	None	-1	5	Human	8.1	pKd	=	8.1	Binding	Mechanism of ActionMechanism of Action	Drug Central		None	None	None		None	None
		1321	1942	0	None	15	3	Human	8.5	pKd	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10051117
		1340	2472	0	None	-	1	Human	10.1	pKd	None	10.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	546	11	0	5	5.7	COc1ccc2c(c1CCCCN1CCN(CC1)C[C@H](c1ccc(cc1)F)N1CCN(CC1)C(C)C)cccc2	12538838
		6918688	2472	0	None	-	1	Human	10.1	pKd	None	10.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	546	11	0	5	5.7	COc1ccc2c(c1CCCCN1CCN(CC1)C[C@H](c1ccc(cc1)F)N1CCN(CC1)C(C)C)cccc2	12538838
		1329	314	0	None	-19	3	Mouse	7.3	pKd	None	7.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9454589
		1328	1943	0	None	10	4	Human	9.5	pKd	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9832440
		7046	216448	0	125I-NDP-MSH	-	1	Human	8.0	pKi	=	8.0	Binding	NoneNone	PDSP KiDatabase	133	0	1	1	1.3	C1CNCC2=CC=CC=C21	None
		None	216310	0	125I-[Nle4,D-Phe7]Alpha-MSH	-93	4	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	961	29	13	12	-1.5	CSCCC(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NCC(=O)O)N	None
		None	217596	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	376	4	0	2	4.9	C1CCC(CC1)C(=O)N2CCCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4	None
		None	217597	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	391	4	1	2	4.8	C1CCC(CC1)NC(=O)N2CCCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4	None
		None	217598	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	365	6	1	2	4.3	CCCCNC(=O)N1CCCN(CC1)C(C2=CC=CC=C2)C3=CC=CC=C3	None
		None	217599	0	UNDEFINED	-	1	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	407	4	1	2	5.0	C1CCC(CC1)NC(=S)N2CCCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4	None
		None	216309	0	125I-NDP-MSH	-70	4	Human	7.7	pKi	=	7.7	Binding	NoneNone	PDSP KiDatabase	299	5	3	6	-0.3	CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O	None
		None	216309	0	125I-[Nle4,D-Phe7]Alpha-MSH	-70	4	Human	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	299	5	3	6	-0.3	CC(C)C(C(C)O)(C(=O)OCC1=CCN2C1C(CC2)O)O	None
		1016	3747	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2561	3747	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2733526	3747	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		5384	3747	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		CHEMBL83	3747	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		DB00675	3747	78	None	-70	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
		2726	919	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		621	919	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		83	919	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		CHEMBL71	919	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		DB00477	919	68	None	-154	72	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
		2247	505	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		249	505	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		2603	505	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		CHEMBL296419	505	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		DB00637	505	81	None	-147	42	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
		176	398	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		2157	398	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		2566	398	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		CHEMBL633	398	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		DB01118	398	66	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
		4189	206922	96	None	-46	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		CHEMBL1559	206922	96	None	-46	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		CHEMBL91	206922	96	None	-46	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
		134611880	277	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		16132265	277	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		3633	277	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		4931	277	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		CHEMBL1201610	277	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		DB01285	277	0	None	-14	5	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central		None	None	None		None	None
		131839615	212636	26	None	1	2	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
		16133835	212636	26	None	1	2	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
		CHEMBL407070	212636	26	None	1	2	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central		None	None	None		CCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)C(C)C	None
		10408	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		10408	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		5329	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		5329	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		9941379	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		9941379	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		CHEMBL2070241	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		CHEMBL2070241	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		DB11653	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	22335602
		DB11653	720	28	None	1	4	Human	9.6	pKi	=	9.6	Binding	Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.Inhibition of <sup>125</sup>I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC<sub>4</sub> receptor.	Guide to Pharmacology		None	None	None		CCCC[C@@H](C(=O)N[C@H]1CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@@H](NC1=O)Cc1[nH]cnc1)Cc1ccccc1)CCCN=C(N)N)Cc1c[nH]c2c1cccc2)C(=O)O)NC(=O)C	31599840
		134611880	277	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		16132265	277	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		3633	277	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		4931	277	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		CHEMBL1201610	277	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		DB01285	277	0	None	-14	5	Human	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8884876
		1321	1942	0	None	15	3	Human	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	9630346
		11993702	3593	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		5416	3593	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		9272	3593	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		CHEMBL3301624	3593	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		DB11700	3593	18	None	1	5	Rat	8.6	pKi	=	8.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		11993702	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		11993702	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		5416	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		5416	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		9272	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		9272	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		CHEMBL3301624	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		CHEMBL3301624	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		DB11700	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	19646498
		DB11700	3593	18	None	-1	5	Human	8.7	pKi	=	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	33137293
		1320	366	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1320	366	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		16162729	366	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		16162729	366	0	None	-3	3	Human	7.7	pKi	None	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		1323	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1323	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		1323	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	2535874
		92432	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		92432	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		92432	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	2535874
		CHEMBL430239	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		CHEMBL430239	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		CHEMBL430239	2688	55	None	-10	3	Human	8.5	pKi	None	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	2535874
		1324	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1324	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		1324	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		16154396	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		16154396	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		16154396	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		16197727	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		16197727	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		16197727	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		44285019	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		44285019	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		44285019	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		57514683	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		57514683	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		57514683	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		91898441	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		91898441	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		91898441	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		CHEMBL441738	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		CHEMBL441738	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		CHEMBL441738	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		DB04931	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		DB04931	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	11101306
		DB04931	302	25	None	-3	4	Human	8.7	pKi	None	8.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	6777774
		1325	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		1325	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491
		6440621	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		6440621	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491
		9898183	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		9898183	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491
		CHEMBL3422426	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10493100
		CHEMBL3422426	3600	14	None	1	7	Human	9.5	pKi	None	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	10657491

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